PIM1-IN-1

PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC 50 s of 7, 5530 and 70 nM for PIM1 , PIM2 , and PIM3 , respectively, inhibits the phosphorylation of BAD, a downstream target of PIM , with an EC 50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity In Vitro PIM1-IN-1 (Compound 42) exhibits antiproliferative activity, with GI 50 of 1.48 µM for melanoma cell line SKMEL-19. PIM1-IN-1 has significant synergistic effect combined with different antitumoral agents in different tumor cell lines. PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: SKMEL19 cells Concentration: 2.5, 5, or 10 µM Incubation Time: 24 hours Result: Regulated cell cycle, induced cell apopsis in SKMEL19 cells. In Vivo PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:PIM1 7 nM (IC 50 ) PIM3 70 nM (IC 50 ) PIM2 5530 nM (IC 50 )

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