RU-SKI 43 - Hhat Inhibitor. CAS# 1043797-53-0 60077 3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid

3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid

CID 2011756 was the most potent of the inhibitors with a cellular EC50 of 10±0

Chemical Name: N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide

133053-19-7

OSI-027 shows robust antitumor activity in several different human xenograft models representing various histologies

RU-SKI 43 - Hhat Inhibitor. CAS# 1043797-53-0 60077 3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acidRU SKI, CAS No. 1043797 53 0, 43 is the first potent and specific small molecule inhibitor of Hedgehog acyltransferase (Hhat), and directly inhibits palmitoylation of the Shh ligand. It was discovered by a high throughput screen using a peptide based assay to monitor Hhat mediated Shh palmitoylation (IC50 ~0. 85 M) . In vitro using purified Hhat and ShhN to analyze the kinetics of compounds inhibition of ShhN palmitoylation, RU SKI 43 behaved as an