| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| PD 0332991 hydrochloride - Palbociclib hydrochloride | Axon 1505
CAS [571189-11-2]
MF C24H29N7O2.2HClMW 520.45
Purity:
99%
Soluble in water
Description
An orally active cyclin-dependent kinase (CDK) inhibitor, specifically targeting on CDK4 and CDK6; a potential agent for the treatment of breast cancer; water soluble hydrochloride salt form, ideal for in vivo experiments. Another salt form, PD 0332991 isethionate (Axon 2052) is also available.
Prime Source Information | | axonmedchem |
| U 73122 | Axon 1225
CAS [112648-68-7]
MF C29H40N2O3MW 464.64
Purity:
99%
Optical purity:
Optically pure
Moderately soluble in DMSO
Description
Phospholipase C (PLC) inhibitor
References
Certificates
Categories
Extra info
Smith et al. U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions. J. Pharmacol. Exp. Ther. 1996, 278, 320.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
PLC
EC 3.1.4.3
PLC inhibitor
Chemical name
1-[6-((8R,9S,13S,14S,17S)-3-Methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-ylamino)-hexyl]-pyrrole-2,5-dione
Parent CAS No.
[112648-68-7]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| CCT 137690 | Axon 1836
CAS [1095382-05-0]
MF C26H31BrN8OMW 551.48
Purity:
98%
Moderately soluble in DMSO
Description
Potent and orally bioavailable Aurora kinase inhibitor, with IC50 values to be 15, 25 and 19 nM for Aurora A, B and C kinases respectively
References
Certificates
Categories
Extra info
V Bavetsias et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J. Med. Chem. 2010, 53(14), 5213-5228.
A Faisal et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol. Cancer Ther. 2011, 10(11), 2115-2123.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora inhibitor (non-specific)
Chemical name
3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)methyl)-5-methylisoxazole
Parent CAS No.
[1095382-05-0]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| VX 680 - MK 0457 | Tozasertib | Axon 1540
CAS [639089-54-6]
MF C23H28N8OSMW 464.59
Purity:
98%
Soluble in DMSO
Description
Potent inhibitor of aurora kinases with Ki values to be 0.6, 18 and 4.6 nM for aurora A, B and C isotypes respectively; inhibiting also ABL (Ki=30 nM) and FLT3 (Ki=30 nM) kinases
References
Certificates
Categories
Extra info
EA Harrington et al. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nature Medicine 10, 262 - 267 (2004)
GM Cheetham et al. Structural basis for potent inhibition of the aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680. Cancer Lett. 2007, 251, 323-329.
FJ Giles et al. MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. Blood 2007, 109, 500-502.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora inhibitor (non-specific)
Chemical name
Cyclopropanecarboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-1H-pyrazol-3-ylamino)-pyrimidin-2
-ylsulfanyl]-phenyl}-amide
Parent CAS No.
[639089-54-6]
Order
Size
Unit Price
Stock
10 mg
€60.00
In Stock | | axonmedchem |
| PF 05105679 | Axon 2483
CAS [1398583-31-7]
MF C26H21FN2O3MW 428.45
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
TRPM8 inhibitor (IC50 value 0.1 μM for TRPM8 in single cell patch clamp electrophysiology (Ephys) studies), showing >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels. Although PF-05105679 shows no effect on core body temperature in humans, it proofs to be a useful tool to study in vitro effects of TRPM8 on thermoregulation and for the treatment of pain in humans.
KEYWORDS: PF 05105679 | supplier | TRPM8 antagonist | PF05105679 | PF5105679 | CAS [1398583-31-7] | TRPM8 | Blocker | Ion Channels | transient receptor potential | TRP | cold | pain | analgesic | thermoregulation | melastatin | hypothermia | | axonmedchem |
| SNS 314 mesylate | Axon 2906
CAS [1146618-41-8]
MF C18H15ClN6OS2.CH4O3SMW 527.04
Purity:
99%
Soluble in DMSO
Description
SNS 314 mesylate is a potent and selective Aurora kinase inhibitor with IC50 values of 9 nM, 31 nM and 3 nM for Aurora A, Aurora B and Aurora C, respectively. Moreover, SNS 314 mesylate displays significant activity in pre-clinical in vivo models.
KEYWORDS: SNS 314 mesylate | supplier | Aurora inhibitor | SNS314 mesylate | SNS-314 mesylate | CAS [1146618-41-8] | [1057249-41-8] | Non Selective (Histone; Survivin; Topo; TPX2) | Aurora | Inhibitor | Enzymes | | axonmedchem |
| GSK 2193874 | Axon 2742
CAS [1336960-13-4]
MF C37H38BrF3N4OMW 691.62
Purity:
98%
Soluble in DMSO
Description
GSK 2193874 is a potent, selective, and orally active TRPV4 channel blocker (IC50 values of 2 and 40 nM for rTRPV4 and hTRPV4, respectively). TRPV4 blockade with GSK 2193874 provided protection against the development of pulmonary edema and the resulting deficits in arterial oxygenation in heart failure models in vivo.
KEYWORDS: GSK 2193874,supplier,TRPV4 antagonist,GSK2193874,GSK-2193874,CAS [1336960-13-4],Non Selective (Cations),TRPV4,Antagonist,Ion Channels,Pulmonary Edema | | axonmedchem |
| A 784168 | Axon 1816
CAS [824982-41-4]
MF C19H15F6N3O3SMW 479.40
Purity:
98%
Soluble in DMSO
Description
Potent and selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptors (IC50: 24 nM); displayed potent anti-nociceptive effects in a broad range of animal pain models upon oral dosing. This analgesic activity results from its ability to penetrate the central nervous system
References
Certificates
Categories
Extra info
M Cui et al. TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J. Neurosci. 2006, 26(37), 9385-9393.
SB Brown et al. Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. Bioorg. Med. Chem. 2008, 16, 8516–8525.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
TRPV1
Unclassified
TRPV1 receptor antagonist
Chemical name
1-(3-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethylsulfonyl)phenyl)-1,2,3,6-tetrahydropyridine-4-carboxamide
Parent CAS No.
[824982-41-4]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| ABT 102 | Axon 1504
CAS [808756-71-0]
MF C21H24N4OMW 348.44
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptors (IC50 values to be 5-7 nM) under clinical trials; TRVP1 receptor antagonism is a promising approach for pain management
References
Certificates
Categories
Extra info
CS Surowy et al. ABT-102 Blocks Polymodal Activation of Transient Receptor Potential Vanilloid 1 Receptors in Vitro and Heat-Evoked Firing of Spinal Dorsal Horn Neurons in Vivo. JPET 2008, 326(3), 879-888.
P Honore et al. Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia. Pain. 2009, 142(1-2), 27-35.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
TRPV1
Unclassified
TRPV1 antagonist
Chemical name
(R)-1-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea
Parent CAS No.
[808756-71-0]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| FG-2216 - YM 311 | Axon 2570
CAS [223387-75-5]
MF C12H9ClN2O4MW 280.66
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally active HIF prolyl 4-hydroxylase inhibitor (P4-HI; IC50 value 3.9 μM for PHD2) that increases plasma EPO levels up to 30-fold in hemodialysis (HD) patients, and reduces cardiac remodeling after myocardial infarction in rats independent of a reduction of collagen maturation or altering growth factors.
KEYWORDS: FG-2216 | supplier | PHD inhibitor | YM 311 | FG2216 | YM311 | CAS [223387-75-5] | Hypoxia-signaling cascade | PHD-2 (HIF1) | PHD-4 (HIF1) | Inhibitor | hypoxia inducible factor | prolyl hydroxylase | EPO | hemodialysis | cardiac remodeling | myocardial infarction | collagen | | axonmedchem |
| Hesperadin | Axon 2096
CAS [422513-13-1]
MF C29H32N4O3SMW 516.65
Purity:
99%
Soluble in DMSO
Description
A rapid, reversible and ATP-competitive inhibitor of Aurora B
References
Certificates
Categories
Extra info
S Hauf et al. The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore–microtubule attachment and in maintaining the spindle assembly checkpoint. J. Cell Biol. 2003, 16192), 281.
F Sessa et al. Mechanism of Aurora B activation by INCENP and inhibition by hesperadin. Mol. Cell, 2005, 18(3), 379.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Reversible and ATP-competitive inhibitor of Aurora B
Chemical name
(Z)-N-(2-oxo-3-(phenyl(4-(piperidin-1-ylmethyl)phenylamino)methylene)indolin-5-yl)ethanesulfonamide
Parent CAS No.
[422513-13-1]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| HIF-2a Translation Inhibitor 76 | Axon 2614
CAS [882268-69-1]
MF C9H9N3O4S2MW 287.32
Purity:
99%
Soluble in DMSO
Description
HIF-2a translation inhibitor (IC50 value 5 µM); Decreases HIF-2a protein and HIF-2a target gene expression in normoxia and hypoxia independent of HIF-2a mRNA expression or HIF-2a protein stability, and independent of mTOR activity. Moreover, the translation inhibitor 76 enhances binding of IRP1 to the HIF-2a IRE (Iron-Responsive Element).
KEYWORDS: HIF-2a Translation Inhibitor 76 | supplier | HIF2a translation inhibitor | CAS [882268-69-1] | DNA-RNA | HIF-2α | Transcription Factor | Iron-Responsive Element | IRE | mTOR | hypoxia | IRP1 | | axonmedchem |
| FG-4592 - Roxadustat | ASP 1517 | Axon 2588
CAS [808118-40-3]
MF C19H16N2O5MW 352.34
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
New-generation oral HIF-PHD inhibitor (IC50 value 591 nM for inhibition of PHD2 in a fluorescence polarization assay) for the treatment of anemia in patients with chronic kidney disease (CKD) by promoting erythropoiesis. FG 4592 (Roxadustat) treatment significantly inhibited tert-Butyl hydroperoxide (TBHP)-induced apoptosis and increases the survival of neuronal PC-12 cells by stabilization of HIF-1α. FG 4592 is also shown to inhibit Fat Mass and Obesity Associated Protein (FTO; IC50 value 9.8 μM).
KEYWORDS: FG-4592 | supplier | HIFα-PHD inhibitor | Roxadustat | ASP 1517 | FG4592 | ASP1517 | CAS [808118-40-3] | Hypoxia-signaling cascade | PHD-2 (HIF1) | Inhibitor | PHD2 | anemia | chronic kidney disease | CKD | erythropoiesis | survival | HIF-1α | Fat | Obesity Associated Protein | FTO | | axonmedchem |
| AMG 900 | Axon 1783
CAS [945595-80-2]
MF C28H21N7OSMW 503.58
Purity:
98%
Soluble in DMSO
Description
Potent and highly selective inhibitor of pan-aurora kinases with activity in taxane-resistant tumor cell lines
References
Certificates
Categories
Extra info
MN Payton et al. Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010, 70(23), 9846-9854.
L Huang et al. In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases. Xenobiotica. 2011, 41(5), 400-408.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora inhibitor (non-specific)
Chemical name
N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine
Parent CAS No.
[945595-80-2]
Order
Size
Unit Price
Stock
5 mg
€115.00
In Stock | | axonmedchem |
| CDIBA | Axon 1609
CAS [479422-22-5]
MF C31H26ClNO3MW 496.00
Purity:
100%
Soluble in DMSO
Description
Potent and selective cytosolic phospholipase A2 (cPLA2) inhibitor
References
Certificates
Categories
Extra info
Novel Target for Existing Drug May Improve Success of Radiation Therapy. ScienceDaily Sep. 20, 2010.
AG Linkous et al. Cytosolic Phospholipase A2 and Lysophospholipids in Tumor Angiogenesis. J. Natl. Cancer Inst. 2010; 102(18), 1398-1412.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Pain & Inflammation
EC 3.1.1.4
PLA2
cPLA2 inhibitor
Chemical name
4-[2-[5-chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]-ethoxy]benzoic acid
Parent CAS No.
[479422-22-5]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| HIF-2 inhibitor 2 - Compound 2 | Axon 2034
CAS [1422955-31-4]
MF C12H6ClFN4O3MW 308.65
Purity:
100%
Soluble in DMSO
Description
Allosteric inhibitor of HIF-2, which selectively antagonizes HIF-2 heterodimerization and DNA-binding activity in vitro and in cultured cells, reducing HIF-2 target gene expression
References
Certificates
Categories
Extra info
TH Scheuermann et al. Allosteric inhibition of hypoxia inducible factor-2 with small molecules. Nat. Chem. Biol. 2013, 9, 271–276.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Epigenetics
Transcription Factors
TF class 1.2
HIF
Allosteric inhibitor of HIF-2
Chemical name
N-(3-chloro-5-fluorophenyl)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine
Parent CAS No.
[1422955-31-4]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| LW6 | Axon 2480
CAS [934593-90-5]
MF C26H29NO5MW 435.51
Purity:
99%
Soluble in DMSO
Description
Novel HIF-1 inhibitor (IC50 value 2.44 μM) that promotes proteasomal degradation of HIF-1α via upregulation of von-Hippel-Lindau (VHL), without affecting the activity of prolyl hydroxylase (PHD). Evidence was found that identified MDH2 as a target protein of LW-6. Moreover, LW6 suppresses angiogenesis by inhibition of HIF-1α stability via direct binding with calcineurin b homologous protein 1 (CHP1) in a Ca2+ dependent manner.
KEYWORDS: LW 6 | supplier | HIF-1 inhibitor | LW6 | CAS [934593-90-5] | DNA-RNA | HIF-1 | CHP1 | Inhibitor | Transcription Factor | hypoxia inducible factor | angiogenesis | tumor | cancer | von-Hippel-Lindau | VHL | prolyl hydroxylase | PHD | calcineurin b homologous protein 1 | endoplasmic reticulum | malate d | | axonmedchem |
| IOX2 | Axon 1921
CAS [931398-72-0]
MF C19H16N2O5MW 352.34
Purity:
100%
Soluble in DMSO
Description
A selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20µM)
References
Certificates
Categories
Extra info
YM Tian et al. Differential sensitivity of hypoxia inducible factor hydroxylation sites to hypoxia and hydroxylase inhibitors. J. Biol. Chem. 2011, 286(15), 13041-13051.
JK Murray et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. J. Comb. Chem. 2010, 12(5), 676-686.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Epigenetics
PHD (HIF)
Transcription Factors
EC 1.14.11.29
Inhibitor of Hypoxia Inducible Factor PHD
Chemical name
2-(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamido)acetic acid
Parent CAS No.
[931398-72-0]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| KRIBB11 | Axon 2538
CAS [342639-96-7]
MF C13H12N6O2MW 284.27
Purity:
99%
Soluble in DMSO
Description
HSF1 inhibitor (IC50 value 1.2 µM for inhibition of heat shock-induced luciferase activity). KRIBB11 blocks the induction of HSF1 downstream target proteins such as HSP27 and HSP70, and induces growth arrest and apoptosis in HCT-116 cells. KRIBB11 inhibits HSF1-dependent recruitment of positive transcription elongation factor b (p-TEFb) to the hsp70 promoter, and tumor growth is inhibited without body weight loss upon intraperitoneal treatment of nude mice with KRIBB11. KRIBB11 enhances the cytotoxicity of nocodazole and parbendazole.
KEYWORDS: KRIBB11 | supplier | HSF1 inhibitor | CAS [342639-96-7] | KRIBB 11 | DNA-RNA | HSF1 | Inhibitor | Transcription Factor | heat sock factor |HSP27 | HSF70 | apoptosis | growth arrest | p-TEFb | | axonmedchem |
| HSF1B | Axon 2101
CAS [1196723-95-1]
MF C26H23Cl2N3OMW 464.39
Purity:
99%
Soluble in DMSO
Description
Human heat shock factor protein (HSF1) activator; close analogue of HSF1A (Axon 1890).
KEYWORDS: HSF1B | 1196723-95-1 | Axon 2101 | HSF1 inhibitor | Axon Ligands | Axon Medchem | Supplier | Axon2101 | HSF1 | Heat shock factor protein | neurodegenerative | Huntington's | poly-glutamine | polyQ | | axonmedchem |
| 10058-F4 | Axon 2222
CAS [403811-55-2]
MF C12H11NOS2MW 249.35
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Small-molecule c-Myc inhibitor that induces cell-cycle arrest at G0/G1 phase in a dose-dependent manner. 10058-F4 targets c-Myc-Max, to disrupt the heterodimer and/or to prevent its formation, and abrogates various c-Myc–dependent functions, and induces myeloid differentiation of human acute myeloid leukemia.
References
Certificates
Categories
Extra info
M.J. Huang et al. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia. Exp. Hematol. 2006, 34, 1480-1489.
H. Wang et al. Improved low molecular weight Myc-Max inhibitors. Mol. Cancer Ther. 2007, 6, 2399-2408.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
c-MYC
Transcription Factors
TF class 1.3.2
Stem Cell Differentiator
c-Myc inhibitor inducing cell-cycle arrest at G0/G1 phase
Chemical name
5-(4-ethylbenzylidene)-2-thioxothiazolidin-4-one
Parent CAS No.
[403811-55-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| YK 4-279 | Axon 2469
CAS [1037184-44-3]
MF C17H13Cl2NO4MW 366.20
Purity:
99%
Soluble in DMSO
Description
Inhibitor of interactions between the fusion protein EWS-FLI1 and RNA helicase A (RHA; Kd value 9.48 µM) with a detrimental effect on ESFT cells both in vitro and in vivo. YK-4-279 is also found to potently inhibit biological activity of ERG (Kd value 11.7 µM) and ETV1 (Kd value 17.4 µM) resulting in suppression of both primary tumor growth and metastasis of fusion positive prostate cancer xenografts. ETV1 is a member of the translocated erythroblastosis virus E26 transforming sequence (ETS) family of transcription factors) and targets MMP7, MMP13, FKBP10 and GLYATL2 genes, among several others.
References
Certificates
Categories
Extra info
S. Rahim et al. A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model. PLoS One. 2014 Dec 5;9(12):e114260.
S. Rahim et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion. PLoS One. 2011 Apr 29;6(4):e19343.
H.V. Erkizan et al. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. Nat Med. 2009 Jul;15(7):750-6.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Oncogene Fusion Proteins
Transcription Factors
Helicase-Primase
ETV1
ERG
TF class 3.5.2.2.4
Inhibitor of ETV1, ERG and interactions of EWS-FLI1 and RNA helicase A
Chemical name
4,7-dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)indolin-2-one
Parent CAS No.
[1037184-44-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| FDI 6 - NCGC 00099374 | Axon 2384
CAS [313380-27-7]
MF C19H11F4N3OS2MW 437.43
Purity:
99%
Soluble in DMSO
Description
Inhibitor of the Forkhead box protein M1 transcription factor (IC50 value 22.5 µM for inhibiting FOXM1-DNA binding). FDI6 displaces FOXM1 from genomic targets in MCF-7 breast cancer cells, and induces concomitant transcriptional downregulation. FDI-6 is inactive against the proteasome, and concordance between its biophysical IC50 and cellular GI50 values (22.5 μM and 18.0 μM, respectively) suggests it does not suffer from the off-target effects of thiostrepton.
References
Certificates
Categories
Extra info
M.V. Gormally et al. Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition. Nat Commun. 2014 Nov 12;5:5165.
G. Marsico et al. Small molecule inhibition of FOXM1: How to bring a novel compound into genomic context. Genomics Data 3 (2015) 19-23.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Transcription Factors
FOXM1
TF class 3.3.1
Inhibitor of the Forkhead box protein M1 (FOXM1)
Chemical name
3-amino-N-(4-fluorophenyl)-6-(thiophen-2-yl)-4-(trifluoromethyl)thieno[2,3-b]pyridine-2-carboxamide
Parent CAS No.
[313380-27-7]
Order
Size
Unit Price
Stock
10 mg
€99.00
In Stock | | axonmedchem |
| FQI 1 | Axon 2157
CAS [599151-35-6]
MF C18H17NO4MW 311.33
Purity:
99%
Soluble in DMSO
Description
Antiproliferative small-molecule inhibitor of α-globin transcription factor CP2 (a.k.a. LSF; IC50 2.1 μM); cell-permeable, potent, specific, and reversible. FQI 1 induces cell death in LSF-overexpressing cells, including Hepatocellular carcinoma (HCC cells). FQI 1 inhibits LSF DNA-binding activity both in vitro and in vivo and also inhibits HCC tumor growth in a mouse xenograft model.
References
Certificates
Categories
Extra info
T.J. Granta et al. Antiproliferative small-molecule inhibitors of transcription factor LSF reveal oncogene addiction to LSF in hepatocellular carcinoma. PNAS 2012, 109, 4503–4508.
H.C. Kang et al. Erythroid Cell-Specific α-Globin Gene Regulation by the CP2 Transcription Factor Family. Mol. Cell. Biol. 2005, 25, 6005–6020.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
CP2
Transcription Factors
TF class 4
Inhibitor of α-globin transcription factor CP2 (LSF)
Chemical name
8-(2-ethoxyphenyl)-7,8-dihydro-[1,3]dioxolo[4,5-g]quinolin-6(5H)-one
Parent CAS No.
[599151-35-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| AS 1842856 | Axon 2839
CAS [836620-48-5]
MF C18H22FN3O3MW 347.38
Purity:
99%
Soluble in DMSO
Description
AS 1842856 is an orally active, potent and selective inhibitor of Forkhead box protein O1 transcription factor (IC50 value of 33 nM). AS 1842856 reduces glucose production through the inhibition of glucose-6 phosphatase and phosphoenolpyruvate carboxykinase mRNA levels in a rat hepatic cell line. Therapeutic drug for treating type 2 diabetes.
KEYWORDS: AS 1842856 | supplier | FOXO1 inhibitor | AS1842856 | AS-1842856 | CAS [836620-48-5] | DNA-RNA | FOXO1 | Inhibitor | Transcription Factors | Diabetes | Forkhead box protein O1 transcription factor | | axonmedchem |
| DiMNF | Axon 1935
CAS [14756-24-2]
MF C21H16O4MW 332.35
Purity:
99%
Soluble in DMSO
Description
Selective aryl hydrocarbon receptor (AHR) modulator (SAhRM)
References
Certificates
Categories
Extra info
IA Murray et al. Suppression of cytokine-mediated complement factor gene expression through selective activation of the Ah receptor with 3',4'-dimethoxy-α-naphthoflavone. Mol. Pharmacol. 2011, 79(3), 508-19.
GA Narayanan et al. Selective Ah receptor modulator mediated repression of CD55 expression induced by cytokine exposure. J. Pharmacol. Exp. Ther. 2012, 2, 345-355.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Diabetes & Metabolism
AHR
Transcription Factors
TF class 1.2
Selective aryl hydrocarbon receptor modulator (SAhRM)
Chemical name
2-(3,4-dimethoxyphenyl)-4H-benzo[h]chromen-4-one
Parent CAS No.
[14756-24-2]
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10 mg
€105.00
In Stock | | axonmedchem |
| HSF1A | Axon 1890
CAS [1196723-93-9]
MF C21H19N3O2S2MW 409.52
Purity:
99%
Soluble in DMSO
Description
Human heat shock factor protein (HSF1) activator; close analogue of HSF1B (Axon 2101).
KEYWORDS: HSF1A | supplier | HSF1 inhibitor | HSF1A | CAS [1196723-93-9] | DNA-RNA | HSF1 | heat shock factor protein | Transcription Factors | neurodegenerative | Huntington | poly-glutamine | polyQ | | axonmedchem |
| HIF Phd Inhibitor 4 | Axon 1948
CAS [1227946-51-1]
MF C21H17ClN4O5SMW 472.90
Purity:
98%
Soluble in DMSO
Description
Inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD)
References
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Example 4 in WO2012059555
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Epigenetics
PHD (HIF)
Transcription Factors
EC 1.14.11.29
Inhibitor of Hypoxia Inducible Factor PHD
Chemical name
N-(4-chlorobenzyl)-3-(5,6-dimethoxypyridin-2-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,2-d]pyrimidine-6-carboxamide
Parent CAS No.
[1227946-51-1]
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Size
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5 mg
€105.00
In Stock | | axonmedchem |
| CID 5951923 | Axon 1863
CAS [749872-43-3]
MF C16H18N2O7SMW 382.39
Purity:
100%
Soluble in DMSO
Description
Inhibitor of the transcription factor Krüppel-like factor 5 (KLF5); significantly reduces endogenous KLF5 protein levels and decreases viability of colon cancer cells, without affecting the nontransformed intestinal epithelial cells IEC-6
References
Certificates
Categories
Extra info
BA Bialkowska et al. Identification of Small-Molecule Inhibitors of the Colorectal Cancer Oncogene Krüppel-like Factor 5 Expression by Ultrahigh-Throughput Screening. Mol. Cancer Ther. 2011, 10(11), 2043-2051.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
KLF5
Transcription Factors
TF class 2.3.2
Inhibitor of Krüppel-like factor 5 (KLF5)
Chemical name
2-[Methyl(tetrahydro-1,1-dioxido-3-thienyl)amino]-2-oxoethyl 3-(3-nitrophenyl)prop-2-enoate
Parent CAS No.
[749872-43-3]
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Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| DMOG | Axon 1977
CAS [89464-63-1]
MF C6H9NO5MW 175.14
Purity:
99%
Soluble in water and DMSO
Description
Cell-permeable HIF prolyl hydroxylase (PHD) inhibitor that enhances HIF-1α and -2α, vascular endothelial growth factor (VEGF), and platelet-endothelial cell adhesion molecule 1 expression in vitro. Moreover, DMOG combined with butyrate synergistically improved osteoblast differentiation and pro-angiogenic responses. DMOG is also known to delay neuronal cell death caused by trophic factor deprivation, and to ameliorate vasorelaxation after cold ischemia and hypochlorite-induced warm reperfusion injury.
References
Certificates
Categories
Extra info
K.M. Woo et al. Synergistic effects of dimethyloxalylglycine and butyrate incorporated into α-calcium sulfate on bone regeneration. Biomaterials. 2015 Jan;39:1-14.
D.J. Lomb et al. Prolyl hydroxylase inhibitors delay neuronal cell death caused by trophic factor deprivation. J Neurochem. 2007 Dec;103(5):1897-906.
E. Baader et al. Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues. Biochem J. 1994 Jun 1;300 ( Pt 2):525-30.
T.M. Asikainen et al. Activation of hypoxia-inducible factors in hyperoxia through prolyl 4-hydroxylase blockade in cells and explants of primate lung. Proc Natl Acad Sci U S A. 2005 Jul 19;102(29):10212-7.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Signaling & Oncology
Epigenetics
PHD (HIF)
Transcription Factors
EC 1.14.11.29
Cell-permeable HIF-PHD inhibitor with pro-angiogenic and -osteogenic properties
Chemical name
methyl 2-(2-methoxy-2-oxoethylamino)-2-oxoacetate
Parent CAS No.
[89464-63-1]
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Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| CCT251236 | Axon 2699
CAS [1693731-40-6]
MF C32H32N4O5MW 552.62
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Highly potent, orally bioavailable inhibitor of the HSF1 stress pathway. CCT251236 displayed the desired balance of in vitro properties, while maintaining excellent cellular activity for inhibition of HSF1-mediated HSP72 induction (IC50 value of 19 nM). Moreover, CCT251236 displayed efficacy in a human ovarian carcinoma xenograft model. Promising chemical probe to investigate the role of HSF1 pathway inhibition and pirin binding in vitro and in vivo.
KEYWORDS: CCT251236 | supplier | HSF1 inhibitor | CCT 251236 | CCT-251236 | CAS [1693731-40-6] | DNA-RNA | HSF1 | Inhibitor | Transcription Factors | HSP72 | Pirin | | axonmedchem |
| AZD 1152-HQPA | Axon 1580
CAS [722544-51-6]
MF C26H30FN7O3MW 507.56
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases. The dihydrogen phosphate prodrug, AZD 1152 (Barasertib), is converted rapidly to active AZD1152-HQPA in plasma
References
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Extra info
RW Wilkinson et al. AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis. Clin. Cancer Res. 2007 13(12), 3682-3688.
N Keen et al. Biological characterisation of AZD1152, a highly potent and selective inhibitor of aurora kinase activity. Clin. Cancer Res. 2005, 11, B220.
E Walsby et al. Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts. Haematologica 2008, 93(5), 662-669.
Y Tao et al. Enhancement of radiation response in p53-deficient cancer cells by the Aurora-B kinase inhibitor AZD1152. Oncogene 2008, 27, 3244-3255.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora B inhibitor
Chemical name
2-[5-(7-{3-[Ethyl-(2-hydroxy-ethyl)-amino]-propoxy}-quinazolin-4-ylamino)-1H-pyrazol-3-yl]-N-(3-fluoro-phenyl)-acetamide
Parent CAS No.
[722544-51-6]
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Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| RQ 00203078 | Axon 2498
CAS [1254205-52-1]
MF C21H13ClF6N2O5SMW 554.85
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Selective, potent, and orally active TRPM8 antagonist (IC50 value 8.3 nM) that demonstrated excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration.
References
Certificates
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Extra info
M. Ohmi et al. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8.
Certificate of Analysis
Material Safety Data Sheet
CNS
Miscellaneous
Pain & Inflammation
Unclassified
TRPM8
Selective, potent, and orally active TRPM8 antagonist with in vivo activity
Chemical name
4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
Parent CAS No.
[1254205-52-1]
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10 mg
€125.00
In Stock | | axonmedchem |
| ZM 447439 | Axon 1541
CAS [331771-20-1]
MF C29H31N5O4MW 513.59
Purity:
99%
Soluble in DMSO
Description
Selective and ATP-competitive inhibitor of Aurora B kinase in vitro, with IC50 values to be 50, 250 and 1000 nM for Aurora B, C and A kinases respectively
References
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Extra info
BB Gadea and JV Ruderman. Aurora kinase inhibitor ZM447439 blocks chromosome-induced spindle assembly, the completion of chromosome condensation, and the establishment of the spindle integrity checkpoint. Mol. Biol. Cell 2005, 16(3), 1305-1318.
AA Dar et al. Aurora Kinase Inhibitors - Rising Stars in Cancer Therapeutics? Mol. Cancer Ther. 2010, 9(2), 268 - 278.
F Girdler et al. Validating Aurora B as an anti-cancer drug target. J. Cell. Sci. 2006, 119, 3664-75.
C Ditchfield et al. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J. Cell. Biol. 2003, 161(2), 267-80.
I Georgieva et al. ZM447439, A novel promising aurora kinase inhibitor, Provokes antiproliferative and proapoptotic effects alone and in combination with Bio- and chemotherapeutic agents... Neuroendocrinol. 2010, 91(2), 121-130.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
EC 2.7.11.1
Aurora
Aurora B inhibitor
Chemical name
N-{4-[6-Methoxy-7-(3-morpholin-4-yl-propoxy)-quinazolin-4-ylamino]-phenyl}-benzamide
Parent CAS No.
[331771-20-1]
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Size
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5 mg
€85.00
In Stock | | axonmedchem |
| M8-B hydrochloride | Axon 2423
CAS [883976-12-3]
MF C22H24N2O3S.HClMW 432.96
Purity:
99%
Soluble in water and DMSO
Description
Selective and potent antagonist of the transient receptor potential melastatin-8 (TRPM8) channel with in vitro and in vivo activity. M8-B blocked cold-induced and TRPM8-agonist-induced activation of TRPM8 channels (IC50 values 7.8 nM, 26.9 nM, and 64.3 nM following activation by cold, icilin or menthol, respectively), and decreased deep body temperature in mice and rats in vivo. M8-B did not block other TRP channels (IC50 > 20 μM).
References
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Extra info
M.C. Almeida et al. Pharmacological blockade of the cold receptor TRPM8 attenuates autonomic and behavioral cold defenses and decreases deep body temperature. J Neurosci. 2012 Feb 8;32(6):2086-99.
Certificate of Analysis
Material Safety Data Sheet
CNS
Miscellaneous
Pain & Inflammation
Unclassified
TRPM8
Selective and potent antagonist of the TRPM8 channel
Chemical name
N-(2-aminoethyl)-N-(4-(benzyloxy)-3-methoxybenzyl)thiophene-2-carboxamide hydrochloride
Parent CAS No.
[884049-35-8]
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Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Clemizole | Axon 2458
CAS [442-52-4]
MF C19H20ClN3MW 325.84
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Inhibitor of the transient receptor potential channel TRPC5 with selectivity over other TRCP channels (IC50 values 9.1 µM, 6.4 µM, 1-1.3 µM, 11.3 µM, and 26.5 µM for TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7). Only weakly affected TRPM3 and TRPM8, and TRPV1-4 at markedly higher concentrations of Clemizole. Clemizole was originally developed as antihistaminergic drug and found to inhibit monoamine reuptake in the brain. Clemizole was also found to exhibit antiviral activity by inhibition of NS4B binding to RNA in HCV.
References
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Extra info
J.M. Richter et al. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Mol Pharmacol. 2014 Nov;86(5):514-21.
T. Nguyen et al. Discovery of a novel member of the histamine receptor family. Mol Pharmacol. 2001 Mar;59(3):427-33.
S. Einav et al. The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors. J Infect Dis. 2010 Jul 1;202(1):65-74.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
Pain & Inflammation
H1
Unclassified
TRPC5
Inhibitor of the transient receptor potential channel TRPC5
Chemical name
1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzo[d]imidazole
Parent CAS No.
[442-52-4]
Order
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Unit Price
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10 mg
€75.00
In Stock | | axonmedchem |
| Optovin | Axon 2374
CAS [348575-88-2]
MF C15H13N3OS2MW 315.41
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Reversible photoactivated TRPA1 agonist (EC50 value 2 μM) that specifically activates TRPA1, but not TRPV1 or TRPM8. Optovin activates human TRPA1 via structure-dependent photochemical reactions with redox-sensitive cysteine residues, and enables control of motor activity in paralyzed extremities by localized illumination in animals. Optovin-treated animals respond to 387-nm (violet) stimuli but not to 485-nm (blue), 560-nm (green) or longer wavelengths.
References
Certificates
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Extra info
O. Fajardo et al. Optopharmacology: a light switch for pain. Nat Chem Biol. 2013 Apr;9(4):219-20.
D. Kokel et al. Photochemical activation of TRPA1 channels in neurons and animals. Nat Chem Biol. 2013 Apr;9(4):257-63.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Unclassified
TRPA1
Reversible photoactivated TRPA1 agonist
Chemical name
5-((2,5-dimethyl-1-(pyridin-3-yl)-1H-pyrrol-3-yl)methylene)-2-thioxothiazolidin-4-one
Parent CAS No.
[348575-88-2]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Wiskostatin | Axon 1804
CAS [253449-04-6]
MF C17H18Br2N2OMW 426.15
Purity:
99%
Soluble in DMSO
Description
Selective, reversible inhibitor of neural Wiskott-Aldrich syndrome protein (N-WASP) that inhibits Arp2/3 (actin-related protein 2/3) activation; belongs to be an actin inhibitor for actin-dependent cellular functions
References
Certificates
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Extra info
G Bompard et al. Inhibition of cytokinesis by wiskostatin does not rely on N-WASP/Arp2/3 complex pathway. BMC Cell Biol. 2008, 9, 42.
CJ Guerriero and OA Weisz. N-WASP inhibitor wiskostatin nonselectively perturbs membrane transport by decreasing cellular ATP levels. Am. J. Physiol. Cell Physiol. 2007, 292(4), C1562-1566.
AM Wegner et al. N-wasp and the arp2/3 complex are critical regulators of actin in the development of dendritic spines and synapses. J. Biol. Chem. 2008, 283(23), 15912-15920.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
Immunology
WASP
Globular Proteins
Inhibitor of neural Wiskott-Aldrich syndrome protein (N-WASP)
Chemical name
1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol
Parent CAS No.
[253449-04-6]
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Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| HTI 286 - SPA 110 | Taltobulin | Axon 1650
CAS [228266-40-8]
MF C27H43N3O4MW 473.65
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent tubulin inhibitor; a synthetic hemiasterlin analogue, which is a potent inhibitor of cell growth with an additional advantage of circumventing the P-glycoprotein-mediated resistance
References
Certificates
Categories
Extra info
F Loganzo et al. HTI-286, a Synthetic Analogue of the Tripeptide Hemiasterlin, Is a Potent Antimicrotubule Agent that Circumvents P-Glycoprotein-mediated Resistance in Vitro and in Vivo. Cancer Res. 2003, 63, 1838.
C Redaelli et al. Synthetic tubulin inhibitor HTI-286 and hepatocellular carcinoma: an in-vitro and and in-vivo study. J. Clin. Oncol. (Meeting Abstracts) 2005, 23(16S), 4201.
BA Hadaschik et al. Targeting prostate cancer with HTI-286, a synthetic analog of the marine sponge product hemiasterlin. Int. J. Cancer. 2008, 122(10), 2368-2376.
Y Matsui et al. Intravesical combination treatment with antisense oligonucleotides targeting heat shock protein-27 and HTI-286 as a novel strategy for high-grade bladder cancer. Mol. Cancer Ther. 2009, 8(8), 2402-2411.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Tubulin
Globular Proteins
Tubulin polymerization inhibitor
Chemical name
(S,E)-2,5-dimethyl-4-((S)-N,3,3-trimethyl-2-((S)-3-methyl-2-(methylamino)-3-phenylbutanamido)butanamido)hex-2-enoic acid
Parent CAS No.
[228266-40-8]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| Myoseverin | Axon 1310
CAS [267402-71-1]
MF C24H28N6O2MW 432.52
Purity:
99%
Soluble in DMSO
Description
A microtuble-binding molecule and reversible inhibitor of tubulin polymerization; potential angiogenesis inhibitor
References
Certificates
Categories
Extra info
GR Rosania et al. Myoseverin, a novel microtubule-binding molecule with novel cellular effects. Nat. Biotechnol. 2000, 18, 307-308.
OD Perez et al. Inhibition and reversal of myogenic differentiation by purine-based microtuble assembly inhibitors. Chem. Biol. 2002, 9, 475-483.
HE Park et al. Myoseverin Is a Potential Angiogenesis Inhibitor by Inhibiting Endothelial Cell Function and Endothelial Progenitor Cell Differentiation. DNA and Cell Biol. 2006, 25(9), 514-522.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Tubulin
Globular Proteins
Tubulin polymerization inhibitor
Chemical name
9-Isopropyl-N*2*,N*6*-bis-(4-methoxy-benzyl)-9H-purine-2,6-diamine
Parent CAS No.
[267402-71-1]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| AZ 23 | Axon 1610
CAS [915720-21-7]
MF C17H19ClFN7OMW 391.83
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective tyrosine kinase (Trk) inhibitor with IC50 to 2 and 8 nM for TrkA and TrkB respectively; AZ-23 showed in vivo TrkA kinase inhibition and efficacy in mice following oral administration; having potential for therapeutic utility in neuroblastoma and multiple other cancer indications.
KEYWORDS: AZ 23 | supplier | TrkA inhibitor | AZ23 |CAS[915720-21-7] | Neurotrophin | Trk | Inhibitor | tyrosine kinase | TrkA | TrkB | neuroblastoma | cancer | | axonmedchem |
| GNF 5837 | Axon 2248
CAS [1033769-28-6]
MF C28H21F4N5O2MW 535.49
Purity:
99%
Soluble in DMSO
Description
Potent, selective, and orally bioavailable tropomyosin receptor kinase (TRK) inhibitor with efficacy in rodent cancer tumor models (IC50 values 11, 9, and 7 nM for TRK A, B and C respectively in cellular Ba/F3 assay). Up to 100% tumor regression was observed in tumor xenografts derived from RIE cells expressing both TRKA and NGF.
References
Certificates
Categories
Extra info
P. Albaugh et al. Discovery of GNF 5837, a selective TRK inhibitor with efficacy in rodent cancer tumor models. ACS Med. Chem. Lett. 2012, 3 (2), 140–145.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
RTK class VII; EC 2.7.10.1
Trk
Potent, selective, and orally bioavailable tropomyosin receptor kinase (Trk) inhibitor
Chemical name
1-(3-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-6-ylamino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
Parent CAS No.
[1033769-28-6]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| GW 441756 | Axon 1251
CAS [504433-23-2]
MF C17H13N3OMW 275.30
Purity:
99%
Moderately soluble in DMSO
Description
Potent and orally active TrkA kinase inhibitor (IC50= 2nM)
References
Certificates
Categories
Extra info
ER Wood et al. Discovery and in vitro evaluation of potent TrkA kinase inhibitors: Oxindole and aza-oxindoles. Bioorg. Med. Chem. Lett. 2004, 14(4), 953-957.
J Wang et al. Cellular Assays for High-Throughput Screening for Modulators of Trk Receptor Tyrosine Kinases. Curr. Chem. Genomics, 2008, 1, 27-33.
EJ Jung et al. Cytosolic accumulation of γH2AX is associated with tropomyosin-related kinase A-induced cell death in U2OS cells. Exp. Mol. Med. 2008, 40(3), 276–285.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
RTK class VII; EC 2.7.10.1
Trk
TrkA inhibitor
Chemical name
3-[1-(1-Methyl-1H-indol-3-yl)-meth-(Z)-ylidene]-1,3-dihydro-pyrrolo[3,2-b]pyridin-2-one
Parent CAS No.
[504433-23-2]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| Combretastatin-A4 - CA 4 | Axon 1233
CAS [117048-59-6]
MF C18H20O5MW 316.35
Purity:
99%
Soluble in DMSO
Description
A potent inhibitor of tubulin polymerization and displays strong inhibitory activity on tumor cell growth
References
Certificates
Categories
Extra info
L Sun et al. Abilities of 3,4-diarylfuran-2-one analogs of combretastatin A-4 to inhibit both proliferation of tumor cell lines and growth of relevant tumors in nude mice. Anticancer Res 2004, 24179-186.
P Dey. Chromatin remodeling, cancer and chemotherapy. Curr. Med. Chem. 2006, 13, 2909-2919.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Tubulin
Globular Proteins
Tubulin polymerization inhibitor
Chemical name
2-Methoxy-5-[(Z)-2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenol
Parent CAS No.
[117048-59-6]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| PD 90780 | Axon 2174
CAS [77422-99-2]
MF C19H14N4O4MW 362.34
Purity:
99%
Soluble in DMSO
Description
A nonpeptide inhibitor of nerve growth factor's binding to the P75 NGF receptor; It binds to NGF, not to the P75 receptor. Differential activity of PD90780 suggests altered NGF-p75NTR interactions in the presence of TrkA.
References
Certificates
Categories
Extra info
K Spiegel et al. PD 90780, a nonpeptide inhibitor of nerve growth factor's binding to the P75 NGF receptor. Biochem. Biophys. Res. Comm. 1995, 217, 488-494.
A Colquhoun et al. Differential activity of the nerve growth factor (NGF) antagonist PD90780 [7-(benzolylamino)-4,9-dihydro-4-methyl-9-oxo-pyrazolo[5,1-b]quinazoline-2-carboxylic acid] suggests altered (...). J. Pharm. Exp. Ther. 2004, 310, 505-511.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
p75 NTR
NF-κB
MAPK
JAK-STAT
PI3K-Akt-mTOR
RTK class VII; EC 2.7.10.1
Inhibitor of NGFs binding to the P75 NGFR
Chemical name
7-benzamido-4-methyl-9-oxo-4,9-dihydropyrazolo[5,1-b]quinazoline-2-carboxylic acid
Parent CAS No.
[77422-99-2]
Order
Size
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Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Dihydroxyflavone, 7,8- - DHF, 7,8- | Axon 2089
CAS [38183-03-8]
MF C15H10O4MW 254.24
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent and selective tyrosine kinase receptor B (TrkB) agonist.
7,8-Dihydroxyflavone imitates Brain-derived neurotrophic factor (BDNF) and acts as a robust TrkB agonist, providing a powerful therapeutic tool for the treatment of various neurological diseases
References
Certificates
Categories
Extra info
SW Jang et al. A selective TrkB agonist with potent neurotrophic activities by 7,8-dihydroxyflavone. Proc. Natl. Acad. Sci. USA 2010, 107, 2687-2692.
R Andero et al. Effect of 7, 8-dihydroxyflavone, a small-molecule TrkB agonist, on emotional learning. Am. J. Psychiatry 2011, 168(2), 163-172.
L Devi & M Ohno. 7, 8-dihydroxyflavone, a small-molecule TrkB agonist, reverses memory deficits and BACE1 elevation in a mouse model of Alzheimer's disease. Neuropsychopharmacol. 2011, 37(2), 434-444.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
RTK class VII; EC 2.7.10.1
Trk
Tyrosine kinase receptor B (TrkB) agonist
Chemical name
7,8-dihydroxy-2-phenyl-4H-chromen-4-one
Parent CAS No.
[38183-03-8]
Order
Size
Unit Price
Stock
10 mg
€55.00
In Stock | | axonmedchem |
| Mps1-IN-2 | Axon 2358
CAS [1228817-38-6]
MF C26H36N6O3MW 480.60
Purity:
98%
Soluble in DMSO
Description
Small-molecule inhibitor of Mps1 kinase (IC50 values 145 nM) with greater than 1000-fold selectivity relative to the 352-member kinase panel, with the major exceptions of Gak and Plk1 (Ambit essay Kd values 12 nM, 140 nM, and 61 nM for Mps1, Gak, and Plk1, respectively). Mps1-IN-2 induces bypass of a checkpoint-mediated mitotic arrest and provides a unique tool to investigate the combined inhibition of Plk1 and Mps1.
References
Certificates
Categories
Extra info
W. Lan et al. A chemical tool box defines mitotic and interphase roles for Mps1 kinase. J. Cell Biol. 2010, 190, 21-24.
N. Kwiatkowski et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat. Chem. Biol. 2010, 6, 359-368.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
MPS1 Kinase
EC 2.7.11.1
EC 2.7.12.1
GAK
PLK
Inhibitor of Mps1 kinase with add-on affinity for Gak and Plk1
Chemical name
9-cyclopentyl-2-(2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenylamino)-5-methyl-8,9-dihydro-5H-pyrimido[4,5-b][1,4]diazepin-6(7H)-one
Parent CAS No.
[1228817-38-6]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| ANA 12 | Axon 2468
CAS [219766-25-3]
MF C22H21N3O3SMW 407.49
Purity:
100%
Soluble in DMSO
Description
Selective TrkB antagonist (IC50 value 45.6 ± 8.4 nM for the high-affinity TetOn-rhTrkB) with anxiolytic and antidepressant activity in mice that inhibits processes downstream of TrkB without altering TrkA and TrkC functions. A valuable tool for studying BDNF/TrkB signaling. ANA-12 is also capable of reversing the diminished self-administration of cocaine in male CocSired rats by means of enhanced BDNF expression.
References
Certificates
Categories
Extra info
M. Cazorla et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest. 2011 May;121(5):1846-57.
F.M. Vassoler et al. Epigenetic inheritance of a cocaine-resistance phenotype. Nat Neurosci. 2013 Jan;16(1):42-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Epigenetics
RTK class VII; EC 2.7.10.1
Trk
Selective TrkB antagonist with anxiolytic and antidepressant activity in mice
Chemical name
N-(2-(2-oxoazepan-3-ylcarbamoyl)phenyl)benzo[b]thiophene-2-carboxamide
Parent CAS No.
[219766-25-3]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| AZ 3146 | Axon 1642
CAS [1124329-14-1]
MF C24H32N6O3MW 452.55
Purity:
99%
Soluble in DMSO
Description
Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor, with IC50 to be 35 nM for human Mps1 and selectivity against 46 out of a panel of 50 other kinases and only four kinases were inhibited by >40%, namely FAK, JNK1, JNK2, and KIT. AZ3146 overrides the spindle checkpoint
References
Certificates
Categories
Extra info
L Hewitt et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1–C-Mad2 core complex. J. Cell Biol. 2010, 190(1), 25-34.
W Lan and DW Cleveland. A chemical tool box defines mitotic and interphase roles for Mps1 kinase. 2010, 190 (1): 21-24.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
MPS1 Kinase
EC 2.7.12.1
MPS1 kinase inhibitor
Chemical name
9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one
Parent CAS No.
[1124329-14-1]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Reversine | Axon 1629
CAS [656820-32-5]
MF C21H27N7OMW 393.49
Purity:
99%
Soluble in DMSO
Description
Reversine induces differentiated myogenic-lineage committed cells to become multipotent mesenchymal progenitor cells; it is a potent mitotic inhibitor of MPS1 kinase, which inhibits the spindle assembly checkpoint in a dose-dependent manner; also acts as A3 adenosine receptor antagonist (Ki: 660 nM) or aurora kinases inhibitor (IC50: 400-500 nM for Aurora A/B/C respectively).
KEYWORDS: Reversine | supplier | MPS1 inhibitor | CAS [656820-32-5] | Non Selective (Mitotic Spindle Checkpoint) | MPS1 Kinase | Inhibitor | Enzymes | | axonmedchem |