HSP (e.g. HSP90)

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HSP (e.g. HSP90) Inhibitors | Activators (21)

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
  • P Natl Acad Sci USA, 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 USA, 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 Chemoth Pharm, 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
S7751 VER155008 VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.
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.
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
  • PLoS Negl Trop Dis, 2014, 8(2):e2699
  • ASN Neuro, 2015, 7(1)
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
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.
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
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.
  • Cancer Cell, 2012, 20(3):400-13
  • PLoS Pathog, 2012, 8(11):e1003048
  • 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
S7751 VER155008 <1 mg/mL 100 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
S1175 BIIB021 <1 mg/mL 64 mg/mL 2 mg/mL
S1163 Onalespib (AT13387) <1 mg/mL 25 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
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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