Bioactivity | UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).IC50 value: 0.7-3.4 uM (Cell assay) [1]Target: IAP inhibitorin vitro: UC-112 also potently inhibits the growth of P-glycoprotein (P-gp)-overexpressed multidrug-resistant cancer cells, strongly activates caspase-3/7 and caspase-9 activities, and selectively downregulates survivin level at a concentration as low as 1 μM. Coincubation of UC-112 with a known proteasome inhibitor Z-Leu-Leu-Leu-CHO (MG-132) rescued survivin inhibition, consistent with the anticipated mechanism of action for UC-112 [1].in vivo: As a single agent, UC-112 strongly inhibits tumor growth and reduces both X chromosome-linked IAP and survivin levels in an A375 human melanoma xenograft model in vivo [1]. | ||||||||||||
Name | UC-112 | ||||||||||||
CAS | 383392-66-3 | ||||||||||||
Formula | C22H24N2O2 | ||||||||||||
Molar Mass | 348.44 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Wang J, et al. Discovery of novel second mitochondria-derived activator of caspase mimetics as selective inhibitor of apoptosis protein inhibitors. J Pharmacol Exp Ther. 2014 May;349(2):319-29. [2]. Qinghui Wang, et al. Synthesis and biological evaluation of indole-based UC-112 analogs as potent and selective survivin inhibitors. Eur J Med Chem |