HSP90 Selective 阻害剤

製品コード 製品名 製品説明 Selective / Pan IC50 / Ki
S1175 BIIB021 BIIB021 is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2. Selective HSP90, Ki: 1.7 nM; HSP90, EC50: 38 nM
S2685 KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. Selective HSP90, IC50: 3.8 nM
S1159 Ganetespib (STA-9090) Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3. Selective HSP90, IC50: 4 nM
S1141 17-AAG (Tanespimycin) 17-AAG (Tanespimycin) is a potent HSP90 inhibitor with IC50 of 5 nM, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Phase 2. Selective HSP90, IC50: 5 nM
S7282 NMS-E973 NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. Selective HSP90, DC50: <10 nM
S1163 Onalespib (AT13387) Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2. Selective HSP90, IC50: 18 nM
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. Selective HSP90, IC50: 24 nM
S2656 PF-04929113 (SNX-5422) PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2. Selective HSP90, Kd: 41 nM
S8039 PU-H71 PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. Selective HSP90, IC50: 51 nM
S1142 17-DMAG (Alvespimycin) HCl 17-DMAG is a potent HSP90 inhibitor with IC50 of 62 nM. Phase 2. Selective HSP90, IC50: 62 nM
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Selective HSP90, Kd: 1.2 μM; HSP90 (N-terminal domain), Kd: 0.78 μM
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM. Selective HSP90α, Kd: 0.48 nM
S7097 HSP990 (NVP-HSP990) NVP-HSP990 (HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. Selective HSP90α, IC50: 0.6 nM; HSP90β, IC50: 0.8 nM
S1069 Luminespib (AUY-922, NVP-AUY922) Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2. Selective HSP90α, IC50: 13 nM; HSP90β, IC50: 21 nM
S7459 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β. Selective HSP90β, IC50: 21 nM
S2639 SNX-2112 (PF-04928473) SNX-2112 (PF-04928473) selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG. Selective HSP90α, Ka: 30 nM; HSP90β, Ka: 30 nM
S7458 VER-49009 VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. Selective HSP90β, IC50: 47 nM
S1498 NVP-BEP800 NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1. Selective HSP90β, IC50: 58 nM
Tags: HSP90 inhibitor | HSP90 cancer | HSP90 activation | HSP90 activity | HSP90 phosphorylation | HSP90 assay | HSP90 mutation
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