Catalog No.: PC-20216Not For Human Use, Lab Use Only.
Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).
Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).
Z271-0326 enhanced the NACK ATPase activity in a manner dependent on the ATP concentration.
Z271-0326 displayed a dose-dependent reduction in colony formation in both OE19 (EC50=3.6 μM) and OE33 (EC50=3.14 μM) cell lines.
Z271-0326 inhibited NACK, Notch1, and MAML1 binding to DNA-bound CSL (CBF-1/RBP-J, Su(H), Lag-1), whereas no effect was observed in CSL binding to DNA.
Z271-0326 significantly inhibited the transcription of Notch target genes in both OE19 and OE33 cell lines, inhibited proliferation by causing cell-cycle arrest and apoptosis in esophageal adenocarcinoma.
Z271-0326 (15 mg/kg, i.p.) showed in vivo efficacy in the inhibition of tumor progression in the OE19 xenograft model.
