PIM1-IN-1

PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC₅₀s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC₅₀ of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity^[1]. IC50 & Target: IC50: 7 nM (PIM1), 5530 nM (PIM2), 70 nM (PIM3)^[1] In Vitro: PIM1-IN-1 (Compound 42) exhibits antiproliferative activity, with GI₅₀ 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^[1].
PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells^[1]. In Vivo: PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice^[1].