TAS4464

Biorbyt

TAS4464 [1848959-10-3]

10

1848959-10-3

Research Use Only

C21H23FN6O6S

506.5073

TAS4464 is a highly potent and selective inhibitor of NEDD8 (IC50 of 0.955 nM). TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibited cullin neddylation and subsequently induced the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IkappaBalpha in human cancer cell lines. TAS4464 showed greater inhibitory effects than those of the known NAE inhibitor MLN4924 both in enzyme assay and in cells.

CCOC1=C(C#CC2C3=C(N=CN=C3N)N(C=2)[C@H]4[C@H](O)[C@H](O)[C@@H](CNS(=O)(N)=O)O4)C(F)=CC=C1

12352200