NVP-AUY922 (Luminespib, AUY922) is a potent and selective HSP90 inhibitor with IC50 of 21 and 7.8 nM for HSP90β and HSP90α, respectively.
NVP-AUY922 weakly inhibits HSP90 family members GRP94 and TRAP-1 (Ki=108 and 53 nM), shows no inhibition of HSP72 ATPase and little or no activity against a range of 13 kinases.
NVP-AUY922 inhibits proliferation of human tumor cells (GI50=2-40 nM), induces G(1)-G(2) arrest and apoptosis.
NVP-AUY922 exhibits in vivo activity against xenograft tumor growth, angiogenesis and metastasis.
