YZ129

Biochem/physiol Actions

YZ129 is an ATP site-targeting Hsp90 inhibitor (IC50 = 29.5 nM against 2.5 nM geldanamycin-FITC for binding human HSP90α) that prevents thapsigargin (1 µM)-induced NFAT nuclear translocation in HeLa cells (IC50 = 820 nM) by blocking HSP90 client calcineurin-mediated NFAT dephosphorylation. YZ129 (5 µM; 24-48 hr) suppresses U87 glioblastoma (GBM) cell migration and proliferation as a result of G2/M arrest and apoptosis induction. Daily intraperitoneal administration is efficacious against U87 xenografts (s.c.; bilateral posterior limbs)-derived tumor growth in mice in vivo.

Other Notes

Product may exist in a Tautomeric Form.