| 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) |
HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis. |
Selective |
HSP90α, IC50: 0.6 nM; HSP90β, IC50: 0.8 nM |
| S1175 |
BIIB021 |
BIIB021 (CNF2024) 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 |
| 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 |
Tanespimycin (17-AAG) |
Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3. |
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 |
| S1069 |
Luminespib (NVP-AUY922) |
Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2. |
Selective |
HSP90α, IC50: 13 nM; HSP90β, IC50: 21 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 |
| S7459 |
VER-50589 |
VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
|
Selective |
HSP90β, IC50: 21 nM |
| S7716 |
Pimitespib (TAS-116) |
Pimitespib (TAS-116) is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). |
Selective |
HSP90α, Ki: 34.7 nM; HSP90β, Ki: 21.3 nM |
| S7122 |
XL888 |
XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
Selective |
HSP90, IC50: 24 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 |
| 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 |
| S7458 |
VER-49009 |
VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
Selective |
HSP90β, IC50: 47 nM |
| S8039 |
Zelavespib (PU-H71) |
Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
Selective |
HSP90, IC50: 51 nM |
| S1498 |
NVP-BEP800 |
NVP-BEP800 (VER82576) 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 |
| S1142 |
Alvespimycin (17-DMAG) HCl |
Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. |
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. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses. |
Selective |
HSP90, Kd: 1.2 μM; HSP90 (N-terminal domain), Kd: 0.78 μM |
