PIM1-IN-1
Names
[ CAS No. ]:
1417630-95-5
[ Name ]:
PIM1-IN-1
Biological Activity
[Description]:
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].
[Related Catalog]:
[Target]
PIM1:7 nM (IC50)
PIM3:70 nM (IC50)
PIM2:5530 nM (IC50)
[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]. Apoptosis Analysis[1] Cell 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[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C25H30N8O2
[ Molecular Weight ]:
474.56