HSP (e.g. HSP90)

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HSP (e.g. HSP90) Inhibitors | Activators (20)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1141 17-AAG (Tanespimycin) 17-AAG (Tanespimycin) 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. Phase 2.
  • Mol Cell, 2013, 50(3):368-78
  • J Exp Med, 2012, 209(2):259-73
  • Proc Natl Acad Sci U S A, 2011, 108(18):7535-40
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 in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-mole
  • Nat Med, 2015, 10.1038/nm.3855
  • Nat Commun, 2014, 5:3361
  • Proc Natl Acad Sci U S A, 2014, 111(15):E1528-37
S1142 17-DMAG (Alvespimycin) HCl 17-DMAG (Alvespimycin) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.
  • Hepatology, 2013, 57(1):70-80
  • Oncotarget, 2014, 5(13):4920-8
  • Mol Oncol, 2013, 7(6):1093-102
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.
  • Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1017
  • Hum Mol Genet, 2015, 10.1093/hmg/ddv136
  • Cancer Chemother Pharmacol, 2014, 74(5):1015-22
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
  • BMC Genomics, 2014, 15(1):263
S7750 KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
S8039 PU-H71 PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
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.
S7459 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
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.
  • PLoS Pathog, 2012, 8(11):e1003048
  • Arthritis Rheum, 2013, 65(8):2102-12
  • PLoS Negl Trop Dis, 2014, 8(2):e2699
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.
  • PLoS One, 2013, 8(4):e59315
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.
S7458 VER-49009 VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
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.
  • Mol Cell Biol, 2013, 33(12):2375-87
S2685 KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.
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.
  • J Biol Chem, 2013, 288(23):16308-20
  • Antimicrob Agents Chemother, 2015, 58(7):4138-44
  • Antimicrob Agents Chemother, 2014, 58(7):4138-44
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
  • J Antimicrob Chemother, 2015, 10.1093/jac/dku549
  • Cell Stress Chaperones, 2015, 20(2):309-19
  • Cell Stress Chaperones, 2015, 20(2):309-19
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.
  • PLoS Pathog, 2012, 8(11):e1003048
  • Cancer Cell, 2012, 20(3):400-13
  • PLoS Negl Trop Dis, 2014, 8(2):e2699

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1141 17-AAG (Tanespimycin) <1 mg/mL 117 mg/mL 5 mg/mL
S1069 Luminespib (AUY-922, NVP-AUY922) <1 mg/mL 93 mg/mL 31 mg/mL
S1142 17-DMAG (Alvespimycin) HCl <1 mg/mL 131 mg/mL <1 mg/mL
S1159 Ganetespib (STA-9090) <1 mg/mL 40 mg/mL <1 mg/mL
S1052 Elesclomol (STA-4783) <1 mg/mL 80 mg/mL <1 mg/mL
S7750 KNK437 <1 mg/mL 15 mg/mL <1 mg/mL
S8039 PU-H71 34 mg/mL 100 mg/mL 100 mg/mL
S7097 HSP990 (NVP-HSP990) <1 mg/mL 75 mg/mL <1 mg/mL
S7459 VER-50589 <1 mg/mL 77 mg/mL 77 mg/mL
S7340 CH5138303 <1 mg/mL 83 mg/mL <1 mg/mL
S1175 BIIB021 <1 mg/mL 64 mg/mL 2 mg/mL
S1163 Onalespib (AT13387) <1 mg/mL 25 mg/mL <1 mg/mL
S7282 NMS-E973 <1 mg/mL 90 mg/mL <1 mg/mL
S7458 VER-49009 <1 mg/mL 77 mg/mL <1 mg/mL
S7122 XL888 <1 mg/mL 100 mg/mL <1 mg/mL
S2639 SNX-2112 (PF-04928473) <1 mg/mL 93 mg/mL 1 mg/mL
S2685 KW-2478 <1 mg/mL 115 mg/mL 3 mg/mL
S2656 PF-04929113 (SNX-5422) <1 mg/mL 104 mg/mL 5 mg/mL
S2713 Geldanamycin <1 mg/mL 100 mg/mL <1 mg/mL
S1498 NVP-BEP800 <1 mg/mL <1 mg/mL 15 mg/mL
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