Pim-Inhibitors-Modulators-生命科学试剂-MedChemExpress.pdf

Pim Pim kinases The PIM kinase, also known as serine/threonine kinase plays an important role in cancer biology and is found in three different isoforms namely PIM-1, PIM-2, and PIM-3. Pim kinases are mainly responsible for cell cycle regulation, antiapoptotic activity and the homing and migration of receptor tyrosine kinases mediated via the JAK/STAT pathway. Pim kinases are over-expressed in various types of tumors and regulate the activation of signaling pathways that are important for tumor cell proliferation, survival and expression of drug efflux proteins. This makes Pim kinases attractive targets for the development of anti-cancer chemotherapeutic drugs. www.MedChemE 1 Pim Inhibitors (1S,3R,5R)-PIM447 dihydrochloride (Z)-SMI-4a ((1S,3R,5R)-LGH447 dihydrochloride) Cat. No.: HY-19322C Cat. No.: HY-16576A (1S,3R,5R)-PIM447 (dihydrochloride) an PIM (Z)-SMI-4a is a poten, selective, cell-permeable inhibitor extracted from patent US 20100056576 A1, and ATP-competitive Pim-1 inhibitor with an compound example 72, has IC values of 0.095 μM IC of 24 μM and a K of 0.6 µM. (Z)-SMI-4a also 50 50 i for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3. inhibits Pim-2 (IC50 of 100 μM), and does not