| 产品名称 | SMI-4a - Kinase - Inhibitors / Activators |
| 产品货号 | 27774-2 |
| 产品价格 | 现货询价，电话：010-67529703 |
| 产品规格 | 50 mg |
| 产品品牌 | bpsbioscience |
| 产品概述 | |
| 产品详情 |
MW: 273.2 Da
CAS Registry #: 438190-29-5
Formula: C11H6F3NO2S
Target: Pim1
Background: The serine/threonine Pim kinases have been suggested to promote the activity of the rapamycin-sensitive mammalian target of rapamycin (mTORC1), which regulates cell growth and survival. Pim kinases are overexpressed in solid cancers and hematologic malignancies, and as such have become targets of small molecule inhibitors to prevent the progression of various cancers. SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK.1 SMI-4a has been found to inhibit prostate cancer cell growth and induce G1 phase cell-cycle arrest in precursor T-cell lymphoblastic leukemia/lymphoma cell lines.
Description: SMI-4a is a potent inhibitor of Pim1 with IC50 = 17 -21 nM. It does not significantly inhibit other serine/threonine- or tyrosine-kinases. It induces G1 phase cell cycle arrest and induces apoptosis through the mitocondrial pathway. It downregulates c-myc and induces p27Kip1 expression. Inhibits PRAS40 phosphorylation and mTOR activity, as well as the mammalian target of rapamycin C1 (mTORC1) pathway. SMI-4a is a potential anti-cancer compound that blocks prostate cancer growth.
Synonym(s): 5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione
Biological Activity: SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested. SIM-4a kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 µM).
Solubility: Soluble in DMSO
Format: white to beige powder
Storage / Stability: Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day. Reference(s): 1. Y.W. Lin, et al.; Blood 115, 824 (2010).
2. F. Zhang, et al.; Cancer Biol. Ther. 8, 846 (2009). 3. Z. Xia, et al.; J.Med.Chem. 52, 74 (2009). Scientific Category: Pim
Product Type: Inhibitor
Data shown is lot-specific. Contact us for specific information on other lots.
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