HSP90 Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
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|
KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.
|Selective||HSP90, IC50: 3.8 nM|
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|
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|
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|
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|
XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
|Selective||HSP90, IC50: 24 nM|
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|
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|
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|
CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
|Selective||HSP90α, Kd: 0.48 nM|
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|
VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
|Selective||HSP90β, IC50: 21 nM|
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|
VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
|Selective||HSP90β, IC50: 47 nM|
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|
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