Chemical Name: 5-[[2-[[(4-Chlorophenyl)methyl]thio]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]thio]-N,N-dimethyl-1H-tetrazole-1-ethanamine hydrochloride
Biological ActivityWS 383 is a potent and reversible DCN1-UBC12 interaction inhibitor (IC50 = 11 nM). The compound displays selectivity for DCN1-UBC12 over inhibition of a panel of kinases. including Bruton's tyrosine kinase (BTK), cyclin-dependent kinases (CDKs) and epidermal growth factor receptor (EGFR). In vitro, WS 383 selectively inhibits cullin-3 neddylation over other cullins, and induces accumulation of p21, p27 and NRF2.
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