| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Dorsomorphin dihydrochloride | Axon 2150
CAS [1219168-18-9]
MF C24H25N5O.2HClMW 472.41
Purity:
99%
Soluble in water and DMSO
Description
Selective inhibitor of BMP signaling; functions through inhibition of BMP type I receptors ALK2, ALK3 and ALK6 and thus blocks BMP-mediated SMAD1/5/8 phosphorylation; Also a AMPK inhibitor (Ki value 109 nM)
* Note: Dorsomorphin free base (Axon 1708) is also available
References
Certificates
Categories
Extra info
PB Yu et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat. Chem. Biol. 2007, 4(1), 33-41.
J Hao et al. Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 2008, 3(8), e2904.
JH Boergermann et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Intl. J. Biochem. Cell Biol. 2010, 42(11), 1802-1807.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
BMP-ALK
Inhibitor of BMP signaling. Inhibits ALK2, 3 and 6
Chemical name
6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine dihydrochloride
Parent CAS No.
[866405-64-3]
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Size
Unit Price
Stock
2 mg
€65.00
In Stock | | axonmedchem |
| UK 356618 - PF 03890101 | Axon 2111
CAS [230961-08-7]
MF C34H43N3O4MW 557.72
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective matrix metalloprotease-3 (MMP-3 aka stromelysin-1) inhibitor (IC50=5.9 nM); >140-fold selective over MMP-1, MMP-2, MMP-9 and MMP-14
References
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Extra info
MJ Fray et al. Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (Stromelysin-1). Bioorg. Med. Chem. Lett. 2001, 11(4), 571-574.
MJ Fray et al. A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J. Med Chem. 2003, 46(16), 3514-3525.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.17
MMP
Pfizer Licensed Products
Potent MMP-3 (aka Stromelysin-1) inhibitor
Chemical name
(R)-N1-((S)-3,3-dimethyl-1-oxo-1-((R)-1-phenylethylamino)butan-2-yl)-N4-hydroxy-2-(3-(2-methylbiphenyl-4-yl)propyl)succinamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[230961-08-7]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| WZ 4003 | Axon 2385
CAS [1214265-58-3]
MF C25H29ClN6O3MW 496.99
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Specific dual inhibitor of NUAK1 (aka ARK5) and NUAK2 (aka SNARK; IC50 values 20 nM and 100 nM, respectively) with no significant inhibitory effect on a panel of 139 other kinases tested, including ten other AMPK-related kinases. WZ4003 suppressed MYPT1 phosphorylation in a dose-dependent manner, and inhibited cell proliferation, invasion and migration in vivo. Although WZ 4003 is a close analogue of WZ 4002 (Axon 1506), it shows no affinity for the EGFR (Kd value 14 µM)
References
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Extra info
S. Banerjee et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.
W Zhou et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009, 462, 1070-1074.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
p53-Tumor Suppression
DNA-damage Response
EC 2.7.11.1
NUAK
Specific dual inhibitor of NUAK1 (ARK5) and NUAK2 (SNARK)
Chemical name
N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)propionamide
Parent CAS No.
[1214265-58-3]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| CP 471474 | Axon 2104
CAS [210755-45-6]
MF C16H17FN2O5SMW 368.38
Purity:
99%
Soluble in DMSO
Description
CP 471474 is a matrix metalloprotease inhibitor with sub-nanomolar affinity for MMP-2 and 13 among a broad range of MMPs (IC50: 1170, 0.7, 16, 13, 0.9 for MMP-1, MMP-2, MMP-3, MMP-9, and MMP-13 respectively). It attenuates early left ventricular dilation after experimental myocardial infarction in mice. Similarly, CP-471474 attenuated both the early inflammatory response and the emphysematous lesions induced by chronic exposure to cigarette smoke in guinea pigs.
References
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Extra info
LA Reiter et al. Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1. Bioorg. Med. Chem. Lett. 2004, 14, 3389-3395.
LE Rohde et al. Matrix metalloproteinase inhibition attenuates early left ventricular enlargement after experimental myocardial infarction in mice. Circulation 1999, 99, 3063-3070.
M Selman et al. Matrix metalloproteinases inhibition attenuates tobacco smoke-induced emphysema in guinea pigs. Chest 2003, 123, 1633-1641.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.24
MMP
Pfizer Licensed Products
MMP inhibitor
Chemical name
2-(4-(4-fluorophenoxy)phenylsulfonamido)-N-hydroxy-2-methylpropanamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[210755-45-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Foretinib - GSK 1363089 | Exel 2880 | XL 880 | Axon 1582
CAS [849217-64-7]
MF C34H34F2N4O6MW 632.65
Purity:
98%
Soluble in DMSO
Description
An orally available inhibitor targeting c-MET (IC50: 0.4 nM) and VEGFR2
References
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Extra info
JP Eder et al. A Phase I Dose-Escalation Study to Assess the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Early Antitumor Activity of Foretinib. Clin. Cancer Res. 2010, 16(13), 3507.
L Liu et al. Novel mechanism of lapatinib resistance in HER2-positive breast tumor cells: activation of AXL. Cancer Res. 2009, 69(17), 6871-8.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
c-MET
RTK class X; EC 2.7.10.1
c-MET and VEGFR2 tyrosine kinase inhibitor
Chemical name
N-(4-(7-(3-morpholinopropoxy)-6-methoxyquinolin-4-yloxy)-3-fluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Parent CAS No.
[849217-64-7]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| TMI 005 - Apratastat | Axon 1507
CAS [287405-51-0]
MF C17H22N2O6S2MW 414.50
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Novel, oral TACE/MMP inhibitor for rheumatoid arthritis; Apratastat (TMI-005) blocks secretion of soluble TNF-α and down regulates multiple MMPs, which have been implicated in cartilage destruction and bone erosions of RA
References
Certificates
Categories
Extra info
MM Thabet and TWJ Huizinga. Apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis. Curr. Opin. Investig. Drugs. 2006, 7(11), 1014-1019.
ML Moss et al. Drug Insight: Tumor Necrosis Factor Converting Enzyme as a Pharmaceutical Target for Rheumatoid Arthritis. Nat. Clin. Pract. Rheumatol. 2008, 4(6), 300.
C Shu et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J. Clin. Pharmacol. 2011, 51(4), 472-481.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Miscellaneous
Pain & Inflammation
TACE
NF-κB
EC 3.4.24.86
TACE/MMP inhibitor
Chemical name
(S)-4-[4-(4-Hydroxy-but-2-ynyloxy)-benzenesulfonyl]-2,2-dimethyl-thiomorpholine-3-carboxylic acid hydroxyamide
Parent CAS No.
[287405-51-0]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| XCT 790 | Axon 2337
CAS [725247-18-7]
MF C23H13F9N4O3SMW 596.42
Purity:
99%
Soluble in DMSO
Description
Estrogen-related receptor α (ERRα) inverse agonist (IC50 value of ~300–500 nM) and potent mitochondrial uncoupler that induces cell death in chemotherapeutic resistant cancer cells by causing mitochondrial dysfunction. XCT790 was found to potently activate AMPK in a dose-dependent and ERRα-independent manner at concentrations more than 25-fold below those typically used to perturb ERRα. Measurements of mitochondrial membrane potential, oxygen consumption, and extracellular acidification rates indicated acute and dose-dependent uncoupling of oxidation from phosphorylation in mitochondria by XCT 790. It modulates the activity of ERRα and reduces the proliferation of various cell lines by blocking the G1/S transition of the cell cycle in an ERRα-dependent manner. XCT 790 showed no activity towards a wide range of (GAL4-chimeric) receptors.
References
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Extra info
B. Eskiocak et al. The estrogen-related receptor α inverse agonist XCT 790 is a nanomolar mitochondrial uncoupler. Biochemistry. 2014 Jul 29;53(29):4839-46.
F. Wu et al. Estrogen-related receptor alpha (ERRalpha) inverse agonist XCT-790 induces cell death in chemotherapeutic resistant cancer cells. Chem Biol Interact. 2009 Oct 7;181(2):236-42.
S. Bianco et al. Modulating estrogen receptor-related receptor-alpha activity inhibits cell proliferation. J Biol Chem. 2009 Aug 28;284(35):23286-92.
O. Lanvin et al. Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-alpha degradation by the estrogen receptor-related receptor-alpha inverse agonist XCT790. J Biol Chem. 2007 Sep 28;282(39):28328-34.
P.J. Willy et al. Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand. Proc Natl Acad Sci U S A. 2004 Jun 15;101(24):8912-7.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Diabetes & Metabolism
Endocrinology
Unclassified
ERRα
NR3B
ERRα inverse agonist and potent mitochondrial uncoupler
Chemical name
3-(4-(2,4-bis(trifluoromethyl)benzyloxy)-3-methoxyphenyl)-2-cyano-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acrylamide
Parent CAS No.
[725247-18-7]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| HL 010183 | Axon 2021
CAS [1429218-03-0]
MF C14H20N6.HClMW 308.81
Purity:
99%
Soluble in DMSO
Description
A metformin derivative exerting a potent anti-tumor effect; HL010183 inhibits proliferation and invasion of Hs578T triple-negative (TN) breast cancer cells; 100 fold more potent than metformin.
KEYWORDS: HL 010183 | supplier | Antitumor agent | HL010183 | HL-010183 | CAS [1429218-03-0] | [1125365-14-1] | Glucose | Homeostasis | AMPK | metformin | anti-tumor | proliferation | Hs578T | breast cancer | | axonmedchem |
| A 769662 | Axon 1466
CAS [844499-71-4]
MF C20H12N2O3SMW 360.39
Purity:
99%
Soluble in DMSO
Description
Potent and selective activator of AMP-activated protein kinase (AMPK) β1 subunit-containing complexes
References
Certificates
Categories
Extra info
B Cool et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metabolism. 2006, 3, 403.
M Sanders et al. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. J. Biol. Chem. 2007, 282, 32539.
O Göransson et al. Mechanism of Action of A-769662, a Valuable Tool for Activation of AMP-activated Protein Kinase. J. Biol. Chem. 2007, 282, 32549-32560.
JW Scott et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. Chem. Biol. 2008, 15, 1220.
JT Treebak et al. A-769662 activates AMPK β1-containing complexes but induces glucose uptake through a PI3 kinase-dependent pathway in mouse skeletal muscle. Am. J. Physiol. Cell Physiol. 2009, 297(4), C1041-C1052.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Stem Cell
AMPK
PI3K-Akt-mTOR
EC 2.7.11.31
AMPK activator
Chemical name
6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl )-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile
Parent CAS No.
[844499-71-4]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| BAM15 | Axon 2736
CAS [210302-17-3]
MF C16H10F2N6OMW 340.29
Purity:
99%
Soluble in DMSO
Description
BAM15 is a mitochondrial protonophore uncoupler, which does not depolarize the plasma membrane. Compared to FCCP, an uncoupler of equal potency, BAM15 treatment of cultured cells stimulates a higher maximum rate of mitochondrial respiration and is less cytotoxic. Furthermore, BAM15 is bioactive in vivo and dose-dependently protects mice from acute renal ischemic-reperfusion injury.
KEYWORDS: BAM15 | supplier | Mitochondrial uncoupler | BAM 15 | BAM-15 | CAS [210302-17-3] | Proton | Ionophore (proton) | Ionophore | Unclassified | | axonmedchem |
| AICAR - Acadesine | NSC 105823 | AICA-riboside | Arasine | Axon 2389
CAS [2627-69-2]
MF C9H14N4O5MW 258.23
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent AMPK activator. AICAR activates AMPK due to increased phosphorylation, causes phosphorylation and inactivation of HMG-CoA reductase, and almost total cessation of fatty acid and sterol synthesis. AICAR causes ZMP (a cellular mimetic of AMP) to accumulate inside the cell but does not perturb the cellular contents of ATP, ADP or AMP, and induces differentiation of acute myeloid leukemia cells, and astroglial differentiation of neural stem cells via activating the JAK/STAT3 pathway independently of AMP-activated protein kinase. AICAR can also significantly up-regulate pluripotency-associated genes and down-regulate differentiation-associated transcription factors.
Caution: Axon Ligands™ are for research purposes only! Not for human consumption!
References
Certificates
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Extra info
J.M. Corton et al. 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? Eur J Biochem. 1995 Apr 15;229(2):558-65.
G.F. Merrill et al. AICA riboside increases AMP-activated protein kinase, fatty acid oxidation, and glucose uptake in rat muscle. Am J Physiol. 1997 Dec;273(6 Pt 1):E1107-12.
Y. Zang et al. AICAR induces astroglial differentiation of neural stem cells via activating the JAK/STAT3 pathway independently of AMP-activated protein kinase. J Biol Chem. 2008 Mar 7;283(10):6201-8.
H. Lalic et al. 5-Aminoimidazole-4-carboxamide ribonucleoside induces differentiation of acute myeloid leukemia cells. Leuk Lymphoma. 2014 Oct;55(10):2375-83.
X. Shi et al. AICAR sustains J1 mouse embryonic stem cell self-renewal and pluripotency by regulating transcription factor and epigenetic modulator expression. Cell Physiol Biochem. 2013;32(2):459-75. doi: 10.1159/000354451. Epub 2013 Aug 27.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Diabetes & Metabolism
Epigenetics
Stem Cell
AMPK
TGF-β
MAPK
PI3K-Akt-mTOR
EC 2.7.11.31
Potent AMPK activator and inducer of differentiation of NSCs
Chemical name
5-amino-1-((2R,3S,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1H-imidazole-4-carboxamide
Parent CAS No.
[2627-69-2]
Order
Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| ZLN 024 | Axon 2445
CAS [723249-01-2]
MF C13H13BrN2OSMW 325.22
Purity:
100%
Soluble in DMSO
Description
Allosteric activator of AMP-activated protein kinase (AMPK; EC50 values 0.42 µM and 0.95 µM for increasing the activity of activated heterotrimers α1β1γ1 and α2β1γ1, respectively) that has no effect on mitochondrial function or the ADP/ATP ratio, and which exerts beneficial metabolic effects in vitro and in vivo. ZLN 024 reduced glucose intolerance and fatty liver characteristics in diabetic db/db mice and provides a promising therapeutic approach for type 2 diabetes mellitus and metabolic syndrome.
References
Certificates
Categories
Extra info
L.N. Zhang et al. Novel small-molecule AMP-activated protein kinase allosteric activator with beneficial effects in db/db mice. PLoS One. 2013 Aug 20;8(8):e72092.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Diabetes & Metabolism
Epigenetics
Stem Cell
AMPK
TGF-β
MAPK
PI3K-Akt-mTOR
EC 2.7.11.31
Allosteric activator of AMP-activated protein kinase (AMPK)
Chemical name
2-(2-(2-bromo-4-methylphenoxy)ethylthio)pyrimidine
Parent CAS No.
[723249-01-2]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| TSE 424 - Bazedoxifene acetate | Viviant | Axon 2051
CAS [198481-33-3]
MF C30H34N2O3.C2H4O2MW 530.65
Purity:
99%
Soluble in DMSO
Description
Third generation selective estrogen receptor modulator (SERM).
This product is also available as its hydrochloride salt (Axon 1748)
References
Certificates
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Extra info
BS Komm et al. Bazedoxifene Acetate: A Selective Estrogen Receptor Modulator with Improved Selectivity. Endocrinology 2005, 146(9), 3999-4008.
DM Biskobing et al. Update on bazedoxifene: A novel selective estrogen receptor modulator. Clin. interv. Aging. 2007, 2(3), 299–303.
SL Silverman et al. Efficacy of Bazedoxifene in Reducing New Vertebral Fracture Risk in Postmenopausal Women With Osteoporosis: Results From a 3-Year, Randomized, Placebo-, and Active-Controlled (...). J. Bone Mineral Res. 2008, 23(12), 1923–1934.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Estrogen (ER)
NR3A
Pfizer Licensed Products
Selective estrogen receptor modulator (SERM)
Chemical name
1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[198481-32-2]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| Endoxifen, (Z)- | Axon 2221
CAS [112093-28-4]
MF C25H27NO2MW 373.49
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
The more active (Z)-isomer of (E/Z)-Endoxifen (Axon 2190), an active metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM; IC50 value 0.01–0.10 μM in estrogen-stimulated proliferation assay in MCF-7 cells); Potently inhibits the growth of estrogen-stimulated BT474 cells. Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Z-Endoxifen may provide a new and better treatment for women with estrogen receptor (ER) positive breast cancer.
References
Certificates
Categories
Extra info
P. Elkins et al. Characterization of the isomeric configuration and impurities of (Z)-endoxifen by 2D-NMR, high resolution LC-MS, and quantitative HPLC analysis. J. Pharm. Biomed. Anal. 2014, 88, 174-179.
J.R. Hawse et al. Endoxifen’s Molecular Mechanisms of Action Are Concentration Dependent and Different than That of Other Anti-Estrogens. PLoS One. 2013, 8, e54613.
A Ahmad et al. Endoxifen, a New Cornerstone of Breast Cancer Therapy: Demonstration of Safety, Tolerability, and Systemic Bioavailability in Healthy Human Subjects. Clin. Pharmacol. Ther. 2010, 88(6), 814–817.
M.D. Johnson et al. Pharmacological Characterization of 4-hydroxy-N-desmethyl Tamoxifen, a Novel Active Metabolite of Tamoxifen. Breast Cancer Research and Treatment 2004, 85, 151-159.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Estrogen (ER)
NR3A
The more active (Z)-isomer of Endoxifen (SERM; Axon 2190)
Chemical name
(Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol
Parent CAS No.
[112093-28-4]
Order
Size
Unit Price
Stock
5 mg
€155.00
In Stock | | axonmedchem |
| Sodium ionophore III - ETH 2120 | Axon 2688
CAS [81686-22-8]
MF C34H52N2O4MW 552.79
Purity:
98%
Soluble in DMSO
Description
Sodium ionophore III is suitable for the assay of sodium activity in blood, plasma, serum, etc. with a solvent polymeric membrane electrode.
KEYWORDS: Sodium ionophore III | supplier | Sodium ionophore | ETH 2120 | ETH-2120 | ETH2120 | CAS [81686-22-8] | Sodium | Ionophore (sodium) | Ionophore | | axonmedchem |
| Endoxifen | Axon 2190
CAS [110025-28-0]
MF C25H27NO2MW 373.49
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM); Potently inhibits the growth of estrogen-stimulated BT474 cells (IC50: 54 nM). Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Drug for the treatment of estrogen receptor (ER) positive breast cancer.The water soluble hydrochloride salt Endoxifen hydrochloride is available as Axon 2707.
KEYWORDS: Endoxifen | supplier | SERM | CAS [110025-28-0] | Estrogen | Selective Estrogen Receptor Modulator | Nuclear receptor | metabolite | ER positive breast cancer | Tamoxifen | | axonmedchem |
| Estetrol | Axon 1926
CAS [15183-37-6]
MF C18H24O4MW 304.38
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO
Description
Estetrol has a relatively moderate affinity for human estrogen α receptor (ERα) and estrogen β receptor (ERβ), with Ki values of 4.9 nmol/l and 19 nmol/l, respectively. Nevertheless, at a concentration of 10 μmol/l, Estetrol shows nearly no affinity for a wide range of >120 other receptors, among them the glucocorticoid, progesterone and testosterone receptors. An estrogen steroid and a metabolite of Estradiol
References
Certificates
Categories
Extra info
Estetrol review: profile and potential clinical applications. HJT Coelingh Bennink et al. Climacteric 2008, 11(Suppl 1), 47-58.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Estrogen (ER)
NR3A
Estrogen receptor agonist, (four- to five-fold preference for the Erα)
Chemical name
(8R,9S,13S,14S,15R,16R,17R)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,15,16,17-tetraol
Parent CAS No.
[15183-37-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| WAY-200070 - WAY-00005 | Axon 2697
CAS [440122-66-7]
MF C13H8BrNO3MW 306.11
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Brain penetrant ERβ-selective agonist (IC50 values 155 nM and 2 nM for ERα and ERβ, respectively) that increases key synaptic proteins in vivo, including PSD-95, synaptophysin and the AMPA-receptor subunit GluR1 and increases dendritic branching and spine number. WAY 20070 regulates hippocampal synaptic plasticity and improve hippocampus-dependent cognition, and shows antidepressant and anxiolytic-like effects in vivo. Potential novel therapeutic agent for the prevention and treatment of photoaging.
KEYWORDS: WAY-200070 | supplier | ERβ agonist | WAY-00005 | WAY200070 | WAY 200070 | WAY00005 | WAY 00005 | CAS [440122-66-7] | Axon Medchem | Axon 2697 | Estrogen | Nuclear Receptor | Brain penetrant | PSD-95 | synaptophysin | AMPA | GluR1 | dendritic branching | synaptic plasticity | cognition | antidepressant | anxiolytic | | axonmedchem |
| Endoxifen hydrochloride | Axon 2707
CAS [1197194-41-4]
MF C25H27NO2.HClMW 409.95
Purity:
99%
Soluble in water and DMSO
Description
Metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM); Potently inhibits the growth of estrogen-stimulated BT474 cells (IC50: 54 nM). Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Drug for the treatment of estrogen receptor (ER) positive breast cancer. Hydrochloride salt of Endoxifen (Axon 2190) which dissolves readily in water and aqueous media.
KEYWORDS: Endoxifen hydrochloride | supplier | Endoxifen | SERM | CAS [1197194-41-4] | [110025-28-0] | Estrogen | Selective Estrogen Receptor (ER) Modulator | Nuclear receptor | metabolite | ER positive breast cancer | Tamoxifen | | axonmedchem |
| BHPI | Axon 2790
CAS [56632-39-4]
MF C21H17NO3MW 331.36
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
BHPI is a potent noncompetitive ERα inhibitor that selectively blocks proliferation of drug-resistant ERα-positive breast and ovarian cancer cells (IC50 values of 27 and 15 nM in MDA-468 and T47D cell lines, respectively). Moreover, BHPI induced rapid and substantial tumor regression in a mouse xenograft model of breast cancer.
KEYWORDS: BHPI | supplier | ER-α antagonist | CAS [56632-39-4] | Estrogen | Estrogen (ER) | Antagonist | Receptors | Breast cancer | | axonmedchem |
| ZB716 | Axon 2652
CAS [1853279-29-4]
MF C32H48BF5O4SMW 634.59
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells. In both tamoxifen-naive and tamoxifen-resistant breast cancer cells, ZB716 potently inhibits cell proliferation and effectively degrades the hormone receptor in a dose-dependent manner. ZB716 is shown to have far superior oral bioavailability in mice when compared to fulvestrant.
* Sold in collaboration with Zenopharm, LLC | | axonmedchem |
| ERB 041 - Prinaberel | Axon 1898
CAS [524684-52-4]
MF C15H10FNO3MW 271.24
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Highly selective estrogen receptor β (ERβ) agonist, with IC50 value of 5.4 nM for human ERβ which is >200-fold selective over Erα
References
Certificates
Categories
Extra info
HA Harris et al. Evaluation of an estrogen receptor-beta agonist in animal models of human disease. Endocrinology 2003, 144(10), 4241-4249.
KF Koehler et al. Reflections on the discovery and significance of estrogen receptor beta. Endocr Rev. 2005, 26(3), 465-478.
XL Wang et al. ERB-041, a selective ER beta agonist, inhibits iNOS production in LPS-activated peritoneal macrophages of endometriosis via suppression of NF-kappaB activation. Mol. Immunol. 2009, 46(11-12), 2413-2418.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Estrogen (ER)
NR3A
Pfizer Licensed Products
Selective estrogen receptor β (ERβ) agonist
Chemical name
2-(3-fluoro-4-hydroxyphenyl)-7-vinylbenzo[d]oxazol-5-ol
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[524684-52-4]
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Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| DPN | Axon 1232
CAS [1428-67-7]
MF C15H13NO2MW 239.27
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Estrogen ERβ agonist
References
Certificates
Categories
Extra info
Harrington et al. Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression. Mol. Cell. Endocrinol. 2003, 206 13.
Montgomery et al. Acute effects of oestrogen receptor subtype-specific agonists on vascular contractility. Br. J. Pharmacol. 2003, 139, 1249.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Estrogen (ER)
NR3A
Estrogen (ER-β) agonist
Chemical name
2,3-Bis-(4-hydroxy-phenyl)-propionitrile
Parent CAS No.
[1428-67-7]
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Size
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10 mg
€70.00
In Stock | | axonmedchem |
| Bazedoxifene hydrochloride - WAY 140424 | TSE 424 hydrochloride | Axon 1748
CAS [198480-56-7]
MF C30H34N2O3.HClMW 507.06
Purity:
98%
Soluble in DMSO
Description
Third generation selective estrogen receptor modulator (SERM).
This product is also available as its acetate salt (Axon 2051)
References
Certificates
Categories
Extra info
DM Biskobing et al. Update on bazedoxifene: A novel selective estrogen receptor modulator. Clin. interv. Aging. 2007, 2(3), 299–303.
SL Silverman et al. Efficacy of Bazedoxifene in Reducing New Vertebral Fracture Risk in Postmenopausal Women With Osteoporosis: Results From a 3-Year, Randomized, Placebo-, (...) J. Bone Mineral Res. 2008, 23(12), 1923–1934.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Endocrinology
Estrogen (ER)
NR3A
Pfizer Licensed Products
Selective estrogen receptor modulator (SERM)
Chemical name
1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol hydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[198481-32-2]
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Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| PPT | Axon 1231
CAS [263717-53-9]
MF C24H22N2O3MW 386.44
Purity:
99%
Soluble in DMSO
Description
Specific estrogen receptor α (ERα) agonist. PPT significantly decreased infarct size in an in vivo rabbit model of ischemia-reperfusion injury.
KEYWORDS: PPT | supplier | ER-α agonist | ER-alpha | Estrogen | CAS [263717-53-9] | Receptor | nuclear | NR3 | ischemia | reperfusion | infarct | cardiac | gene | transrepression | transactivation | | axonmedchem |
| PD 166793 | Axon 1271
CAS [199850-67-4]
MF C17H18BrNO4SMW 412.30
Purity:
99%
Optical purity:
>98% ee
Soluble in 0.1N NaOH(aq), DMSO, and Ethanol
Description
Matrix metalloproteinase (MMP) inhibitor
References
Certificates
Categories
Extra info
H León et al. Inhibition of matrix metalloproteinases prevents peroxynitrite-induced contractile dysfunction in the isolated cardiac myocyte. Br. J. Pharmacol. 2008, 153(4), 676-683.
MM Sung et al. Matrix metalloproteinase-2 degrades the cytoskeletal protein α-actinin in peroxynitrite mediated myocardial injury. J. Mol. Cel. Cardiol. 2007, 43(4), 429-436.
AL Chancey et al. Effects of Matrix Metalloproteinase Inhibition on Ventricular Remodeling Due to Volume Overload. Circulation 2002, 105, 1983-1988.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.24
MMP
MMP inhibitor
Chemical name
(S)-2-(4'-Bromo-biphenyl-4-sulfonylamino)-3-methyl-butyric acid
Parent CAS No.
[199850-67-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| ITD-1, (+)- | Axon 2467
CAS [1409968-46-2]
MF C27H29NO3MW 415.52
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
More active (+)-enantiomer of ITD 1 (Axon 2323), a selective inhibitor of TGFβ/Smad signaling (IC50 values 0.46 μM and 6.90 μM for (+)-ITD 1 and (−)-ITD 1, respectively for TGF-β inhibition) that acts by clearing the type II TGFβ receptor from the cell surface. ITD 1 stimulates the differentiation of cardiomyocytes and promote cardiogenesis in murine embryonic stem cell (mESCs). TGFβ inhibition by the (+)-enantiomer is approximately 15-fold more effective than by its (−)-enantiomer.
KEYWORDS: (+)-ITD-1 | supplier | TGF-βR2 inhibitor | ITD1 | (+)-ITD1 | CAS [1409968-46-2] | [1099644-42-4] | [1217467-13-4] | TGF-β | TGF-βR | Antagonist | active enantiomer | Smad | differentiation | cardiomyocytes | cardiogenesis | mESC | stem cell | | axonmedchem |
| PF 00356231 | Axon 1181
CAS [766536-21-4]
MF C25H20N2O3SMW 428.50
Purity:
98%
Optical purity:
>98% ee
Moderately soluble in DMSO
Description
MMP-12 inhibitor, more active enantiomer
References
Certificates
Categories
Extra info
R Morales et al. Crystal Structures of Novel Non-peptidic, Non-zinc Chelating Inhibitors Bound to MMP-12. J. Mol. Biol. 2004, 341(4), 1063-1076.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.65
MMP
MMP-12 inhibitor
Chemical name
(R)-3-Phenyl-3-{[4-(4-pyridin-4-yl-phenyl)-thiophene-2-carbonyl]-amino}-propionic acid
Parent CAS No.
[766536-21-4]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| ITD 1 | Axon 2323
CAS [1099644-42-4]
MF C27H29NO3MW 415.52
Purity:
98%
Soluble in DMSO
Description
Selective inhibitor of TGFβ/Smad signaling (IC50 value 0.85 μM; 83% TGF-β inhibiton at 2.5 μM) that acts by clearing the type II TGFβ receptor from the cell surface. ITD1 stimulates the differentiation of cardiomyocytes and promote cardiogenesis in murine embryonic stem cell (mESCs). TGFβ inhibition by the (+)-eneatiomer is approximately 15-fold more effective than by its (−)-enantiomer.
Note | | axonmedchem |
| SB 505124 | Axon 2197
CAS [694433-59-5]
MF C20H21N3O2MW 335.40
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective inhibitor of TGF-β type I receptors ALK4 and ALK5 (IC50 values 129 nM and 47 nM, respectively). SB 505124 also inhibits the closely related ALK7 receptor, but not the BMP activated receptors (ALK1, 2, 3, and 6). It inhibits downstream TGF-β and Activin induced signaling of Smad2, but not BMP induced signaling of Smad1, -5, or -8. Pretreatment of the cells with SB-505124 blocked TGFβ–induced cell death but had no effect on TNFα–induced toxicity. Additionally, SB-505124 blocks activation of TGFβ induced MAPK pathways but is ineffective when these pathways are induced by EGF.
References
Certificates
Categories
Extra info
S. DaCosta Byfield et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol. Pharmacol. 2004, 65, 744-52.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
TGF-βR
Selective inhibitor of TGF-β type I receptors ALK4 and ALK5
Chemical name
2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine
Parent CAS No.
[694433-59-5]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| GW 788388 | Axon 1832
CAS [452342-67-5]
MF C25H23N5O2MW 425.48
Purity:
99%
Soluble in DMSO
Description
Potent, orally active and selective inhibitor of transforming growth factor β receptor I (TGF-βR1) (activin receptor-like kinase 5, ALK5).
KEYWORDS: GW 788388 | supplier | ALK5 inhibitor | GW788388 | GW-788388 | CAS [452342-67-5] | TGF-β | TGF-βR | Antagonist | Receptors | | axonmedchem |
| A 77-01 | Axon 1744
CAS [607737-87-1]
MF C18H14N4MW 286.33
Purity:
99%
Soluble in DMSO
Description
Potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. A-77-01 is a close analogue of A-83-01 (Axon 1421) and has a very similar biological profile of A-83-01. A-83-01 is found to decompose to A-77-01 under certain circumstances and A-77-01 is likely an active component or metabolite of its prodrug A-83-01.
KEYWORDS: A 77-01 | supplier | ALK5 inhibitor | A77-01 | A7701 | CAS [607737-87-1] | TGF-β | TGF-beta | RSTK | Enzyme Linked Receptors | activin-like kinase | metabolite | A-83-01 | | axonmedchem |
| Genipin | Axon 1443
CAS [6902-77-8]
MF C11H14O5MW 226.23
Purity:
99%
Soluble in DMSO and Ethanol
Description
Active medication to relieve the symptoms of type 2 diabetes. Genipin stimulates insulin secretion in UCP2-dependent manner (Uncoupling protein 2). Genipin is a protein, collagen, gelatin, and chitosan cross-linker
References
Certificates
Categories
Extra info
LE Parton et al. Glucose sensing by POMC neurons regulates glucose homeostasis and is impaired by obesity. Nature 2007, 449, 228-233.
C Zhang et al. Genipin inhibits UCP2-mediated proton leak and acutely reverses obesity- and high glucose-induced B cell dysfunction in isolated pancreatic islets. Cell Metab. 2006, 3, 417-427.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Miscellaneous
UCP2
Endocrinology
MACP
Protein cross-linker; stimulates insulin secretion
Chemical name
(1R,4aS,7aS)-1-Hydroxy-7-hydroxymethyl-1,4a,5,7a-tetrahydro-cyclopenta[c]pyran-4-carboxylic acid methyl ester
Parent CAS No.
[6902-77-8]
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Size
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Stock
10 mg
€55.00
In Stock | | axonmedchem |
| CCT 031374 hydrobromide | Axon 2161
CAS [1219184-91-4]
MF C23H19N3O.HBrMW 434.33
Purity:
98%
Soluble in DMSO
Description
Inhibitor of TCF-dependent transcription of genes of Wnt signaling pathway with in vivo activity in SW480 colon cancer cells (IC50 of 6.1 μM in a HEK293-based reporter cell line). CCT 031374 acts at the β-catenin level based on the observation that it blocked the nuclear β-catenin/transcription factor (TCF) transcription complex dependent transcription induced by a stabilized form of β-catenin, but not by a constitutively active TCF-VP16 fusion protein.
References
Certificates
Categories
Extra info
K. Ewan et al. A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. Cancer Res. 2010, 70, 5963-5673.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
β-Catenin
Wnt-β-Catenin
Wnt
Inhibitor of TCF-dependent transcription of genes of Wnt signaling pathway
Chemical name
1-biphenyl-4-yl-2-(2,3-dihydro-benzo[d]imidazo[1,2-a]imidazol-9-yl)-ethanone hydrobromide
Parent CAS No.
[442535-46-8]
Order
Size
Unit Price
Stock
2 mg
€60.00
In Stock | | axonmedchem |
| Azoramide | Axon 2567
CAS [932986-18-0]
MF C15H17ClN2OSMW 308.83
Purity:
99%
Soluble in DMSO
Description
Small-molecule modulator of the unfolded protein response (UPR) with antidiabetic activity (IC50 value 8.826 µM for azoramide-induced increase of ASGR-Cluc secretion in HuH7 cells). Azoramide is a dual-function ER modulator that improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress. Moreover, Azoramide improves insulin sensitivity and pancreatic β-cell function in multiple obese mouse preclinical models.
KEYWORDS: Azoramide | supplier | UPR modulator | CAS [932986-18-0] | Unfolded Protein Response | endoplasmatic reticulum | ER stress | protein folding | PERK | IRE1 | ATF6 | obesity | antidiabetic | glucose | | axonmedchem |
| FH535 | Axon 2686
CAS [108409-83-2]
MF C13H10Cl2N2O4SMW 361.20
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Small-molecule dual inhibitor of peroxisome proliferator-activated receptor (PPAR) and Wnt/β-catenin/TCF/LEF signaling. FH535 inhibits recruitment of the coactivators β-catenin and GRIP1, but not the corepressors NCoR and SMRT. FH535 is selectively toxic to carcinomas expressing the Wnt/β-Catenin pathway, and known to inhibit invasion, migration, and growth in vitro in multiple types of cancer, such as liver cancer and triple negative breast cancer cell lines. The water soluble sodium salt of FH535 is available as Axon 2706.
KEYWORDS: FH535 | supplier | Dual Wnt/β-catenin and PPAR inhibitor | FH-535 | FH 535 | CAS [108409-83-2] | Metabolism | PPARγ | PPARδ | peroxisome proliferator–activated receptor | Nuclear | NR1C | Tcf/Lef | | axonmedchem |
| FH535 sodium salt | Axon 2706
CAS [N.A.]
MF C13H9Cl2N2NaO4SMW 383.18
Purity:
99%
Soluble in water and DMSO
Description
Small-molecule dual inhibitor of peroxisome proliferator-activated receptor (PPAR) and Wnt/β-catenin/TCF/LEF signaling. FH535 inhibits recruitment of the coactivators β-catenin and GRIP1, but not the corepressors NCoR and SMRT. FH535 is selectively toxic to carcinomas expressing the Wnt/β-Catenin pathway, and known to inhibit invasion, migration, and growth in vitro in multiple types of cancer, such as liver cancer and triple negative breast cancer cell lines; water soluble sodium salt form of FH535 (Axon 2686).
KEYWORDS: FH535 sodium salt | supplier | Dual Wnt/β-catenin and PPAR inhibitor | FH-535 sodium salt | FH 535 sodium salt | CAS [108409-83-2] | Metabolism | PPARγ | PPARδ | peroxisome proliferator–activated receptor | Nuclear | NR1C | Tcf/Lef | | axonmedchem |
| ISRIB - trans-ISRIB | Axon 2278
CAS [1597403-47-8]
MF C22H24Cl2N2O4MW 451.34
Purity:
99%
Optical purity:
Relative stereochemistry
Soluble in DMSO and DCM-MeOH
Description
First reported, potent and selective inhibitor of the ‘integrated stress response’ (ISR) and a potent inhibitor of PERK signaling. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50 value of 5 nM for inhibition of ATF4-luciferase reporter).Trans-ISRIB reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress, and proved to be 100-fold more potent than cis-ISRIB, indicating that the compound’s interaction with its cellular target is stereospecific.
References
Certificates
Categories
Extra info
C. Sidrauski et al. Pharmacological brake-release of mRNA translation enhances cognitive memory. eLife 2013, 2, e00498.
A.G. Hinnebusch et al. Cell biology. Blocking stress response for better memory? Science. 2015 May 29;348(6238):967-8.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
CNS
PERK
EC 2.7.11.1
Potent inhibitor of the integrated stress response and PERK signaling
Chemical name
N,N'-((1r,4r)-cyclohexane-1,4-diyl)bis(2-(4-chlorophenoxy)acetamide)
Parent CAS No.
[1597403-47-8]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Apoptozole | Axon 2251
CAS [1054543-47-3]
MF C33H25F6N3O3MW 625.56
Purity:
100%
Soluble in DMSO
Description
An apoptosis-inducing small molecule that inhibits the ATPase activity of heat shock cognate 70 (Hsc70) and Hsp70 by binding to its ATPase domain (Kd values 0.21 and 0.14 μM for Hsc70 and Hsp70, respectively as determined by surface plasmon resonance (SPR) spectroscopy). Apoptozole has high cellular potency to restore the chloride channel activity of mutant CFTR by promoting its membrane trafficking.
References
Certificates
Categories
Extra info
H.J. Cho et al. A small molecule that binds to an ATPase domain of Hsc70 promotes membrane trafficking of mutant cystic fibrosis transmembrane conductance regulator. J. Am. Chem. Soc. 2011, 133, 20267-20276.
D.R. Williams et al. An apoptosis-inducing small molecule that binds to heat shock protein 70. Angew. Chem. Int. Ed. Engl. 2008, 47, 7466-7469.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Pain & Inflammation
Hsp70
Ubiquitin
Hsc70
EC 3.6.1
Inhibitor of ATPase activity of Hsc70 and Hsp70
Chemical name
4-((2-(3,5-bis(trifluoromethyl)phenyl)-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl)methyl)benzamide
Parent CAS No.
[1054543-47-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| GSK 2606414 | Axon 2233
CAS [1337531-36-8]
MF C24H20F3N5OMW 451.44
Purity:
99%
Soluble in DMSO
Description
Potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK or EIF2AK3) with IC50 value of 0.4 nM and >1000 fold selectivity over EIF2AK1 (HRI) and EIF2AK2 (PKR). Overall, good selectivity was observed, with only 20 protein kinases inhibited >85% by GSK 2606414 at 10 μM during screening against a panel of 294 kinases. It inhibits the growth of a human tumor xenograft in mice with good oral bioavailability and blood-brain barrier penetration.PERK is a type I ER membrane protein and one of three primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis.
References
Certificates
Categories
Extra info
J.M. Axten et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of PERK (...). J. Med. Chem. 2012, 55, 7193-7207.
J.A. Moreno et al. Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice. Science Translational Medicine 2013, 5(206), 206ra138.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
PERK
EC 2.7.11.1
Potent and selective inhibitor of PERK (EIF2AK3)
Chemical name
1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone
Parent CAS No.
[1337531-36-8]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| ML346 - CID 767276 | Axon 2703
CAS [100872-83-1]
MF C14H12N2O4MW 272.26
Purity:
100%
Soluble in DMSO
Description
ML346 is an activator of Hsp70 (EC50 value of 4.6 μM; HeLa cell toxicity assay). ML346 induces HSF-1-dependent chaperone expression and restores protein folding in conformational disease models. These effects are mediated by novel mechanisms involving FOXO, HSF-1, and Nfr-2. ML346 has good chemical stability, is not reactive with excess glutathione, and is cell permeable.
KEYWORDS: ML346 | supplier | Hsp70 activator | CID 767276 | ML 346 | ML-346 | CID767276 | CID-767276 | CAS [100872-83-1] | CAS [1423118-63-1] | Unfolded Protein Response (Non Selective) | Hsp70 | Activator | Enzymes | ARE | Heat Shock Response | HSR | Probe | Proteostasis | HSF-1 | | axonmedchem |
| SD 208 | Axon 1387
CAS [627536-09-8]
MF C17H10ClFN6MW 352.75
Purity:
99%
Soluble in DMSO
Description
Transforming growth factor β receptor I (TGF-βR I) kinase inhibitor
References
Certificates
Categories
Extra info
M Uhl et al. SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res. 2004, 64, 7954-7961.
SY Leung et al. Effect of TGF-β receptor I kinase inhibitor, SD-208, in chronic allergic airway inflammation and remodeling. J. Pharmacol. Eexp. Ther. 2006, 106, 109314.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
TGF-βR
TGF-βR 1 inhibitor
Chemical name
[2-(5-Chloro-2-fluoro-phenyl)-pteridin-4-yl]-pyridin-4-yl-amine
Parent CAS No.
[627536-09-8]
Order
Size
Unit Price
Stock
2 mg
€60.00
In Stock | | axonmedchem |
| A-92 | Axon 2720
CAS [1448693-69-3]
MF C19H18N10OMW 402.41
Purity:
99%
Soluble in DMSO
Description
A-92 inhibits the stress response of general control nonderepressible 2 kinase (GCN2 or EIF2AK4) (IC50 value of <0.3 μM). Possible chemotherapeutic drug for the treatment of cancer.
KEYWORDS: A-92 | supplier | GCN2 inhibitor | A92 | A 92 | CAS [1448693-69-3] | Unfolded Protein Response (EIF2 Selective) | GCN | Inhibitor | Enzymes | GCN2 | eIF2α | EIF2AK4 | General Control Nonderepressible 2 Kinase | tRNA | | axonmedchem |
| Rbin-2 - Ribozinoindole-2 | Axon 2712
CAS [2032282-97-4]
MF C13H11BrN4SMW 335.22
Purity:
98%
Soluble in DMSO
Description
Rbin-2 (ribozinoindole-2) is a potent, reversible, and specific inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family (GI50 value 14 nM in wild-type cells). Rbin-2 is a chemical probe for the eukaryotic ribosome assembly.
Also Midasin inhibitor Rbin-1 (Axon 2663) is available.
KEYWORDS: Rbin-2 | supplier | Midasin inhibitor | Ribozinoindole-2 | Rbin2 | Rbin 2 | Ribozinoindole2 | Ribozinoindole 2 | CAS [2032282-97-4] | ATP | ATPase (Midasin) | Inhibitor | Enzymes | | axonmedchem |
| Rbin-1 - Ribozinoindole-1 | Axon 2663
CAS [328023-11-6]
MF C13H12N4SMW 256.33
Purity:
99%
Soluble in DMSO
Description
Rbin-1 (ribozinoindole-1) is a potent, reversible, and specific inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family (GI50 value 136 nM in wild-type cells). Rbin-1 is a chemical probe for the eukaryotic ribosome assembly.
Midasin inhibitor Rbin-2 (Axon 2712) is also available.
KEYWORDS: Rbin-1 | supplier | Midasin inhibitor | Ribozinoindole-1 | Rbin1 | Rbin 1 | Ribozinoindole1 | Ribozinoindole 1 | CAS [328023-11-6] | ATP | ATPase (Midasin) | Inhibitor | Enzymes | | axonmedchem |
| Rbin-1 - Ribozinoindole-1 | Axon 2663
CAS [328023-11-6]
MF C13H12N4SMW 256.33
Purity:
99%
Soluble in DMSO
Description
Rbin-1 (ribozinoindole-1) is a potent, reversible, and specific inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family (GI50 value 136 nM in wild-type cells). Rbin-1 is a chemical probe for the eukaryotic ribosome assembly.
Midasin inhibitor Rbin-2 (Axon 2712) is also available.
KEYWORDS: Rbin-1 | supplier | Midasin inhibitor | Ribozinoindole-1 | Rbin1 | Rbin 1 | Ribozinoindole1 | Ribozinoindole 1 | CAS [328023-11-6] | ATP | ATPase (Midasin) | Inhibitor | Enzymes | | axonmedchem |
| STA 9090 - Ganetespib | Axon 1968
CAS [888216-25-9]
MF C20H20N4O3MW 364.40
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Hsp90 inhibitor; exhibits potent antitumor activity and a superior safety profile for cancer therapy; with potent in vitro and in vivo activity in tumor cells harboring constitutively active JAK/STAT signaling.
KEYWORDS: STA 9090 | supplier | HSP90 inhibitor | Ganetespib | STA9090 | CAS [888216-25-9] | Axon Medchem | Axon 1968 | Unfolded Protein Response (Non Selective) | Hsp90 | Inhibitor | Enzymes | | axonmedchem |
| PU-H71 trihydrochloride | Axon 1856
CAS [N.A.]
MF C18H21IN6O2S.3HClMW 621.75
Purity:
99%
Soluble in water
Description
Potent inhibitor of heat shock protein 90 (Hsp90) with IC50 of 51 nM; inhibits cell growth in a range of breast cancer cell lines; inhibit cell proliferation and induce apoptosis in triple-negative breast cancer (TNBC) cells.
Note: On the developers request, this product is not for sale for our customers in the United States.
References
Certificates
Categories
Extra info
SK Moulick et al. Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90. Nature Chem. Biol. 2011, 7, 818–826.
E Caldas-Lopes et al. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc. Natl. Acad. Sci. USA 2009, 106, 8368.
H He et al. Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90. J. Med. Chem. 2006, 49(1), 381-90.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
Hsp90
EC 3.6
Hsp90 inhibitor
Chemical name
8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine trihydrochloride
Parent CAS No.
[873436-91-0]
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5 mg
€105.00
In Stock | | axonmedchem |
| Irestatin 9389 | Axon 1656
CAS [626221-47-4]
MF C16H13F3N4OS2MW 398.43
Purity:
99%
Soluble in DMSO
Description
A potent inhibitor of the endonuclease IRE1 (IC50 = 6.3 nM) and unfolded protein response (UPR)
References
Certificates
Categories
Extra info
D Feldman and AC Koong. Irestatin, a potent inhibitor of IRE1α and the unfolded protein response, is a hypoxia-selective cytotoxin and impairs tumor growth. J. Clin. Oncol. (2007 ASCO Ann. Meeting Proc. PI) 2007, 25 (18S), 3514.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
EC 2.7.11.1
IRE
Endonuclease
IRE1 inhibitor; UPR inhibitor
Chemical name
2-(3-cyano-4-(trifluoromethyl)-6,7-dihydro-5H-cyclopenta[b]pyridin-2-ylthio)-N-(4-methylthiazol-2-yl)acetamide
Parent CAS No.
[626221-47-4]
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10 mg
€125.00
In Stock | | axonmedchem |
| VER 155008 | Axon 1608
CAS [1134156-31-2]
MF C25H23Cl2N7O4MW 556.40
Purity:
99%
Soluble in DMSO
Description
Inhibitor of Heat Shock Protein 70 (Hsp70)
References
Certificates
Categories
Extra info
AJ Massey et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother. Pharmacol. 2010, 66(3), 535-545.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
Hsp70
EC 3.6
Hsp70 inhibitor
Chemical name
4-((((2R,3S,4R,5R)-5-(6-amino-8-(3,4-dichlorobenzylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)methyl)benzonitrile
Parent CAS No.
[1134156-31-2]
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5 mg
€95.00
In Stock | | axonmedchem |