HSP (e.g. HSP90)

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HSP (e.g. HSP90) Inhibitors | Activators (18)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
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.
  • 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 AUY922 (NVP-AUY922) AUY922 (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.
  • Nat Commun, 2014, 5:3361
  • Proc Natl Acad Sci U S A, 2014, 111(15):E1528-37
  • PLoS Pathog, 2012, 8(11):e1003048
S1142 17-DMAG (Alvespimycin) HCl 17-DMAG is a potent, water-soluble HSP90 inhibitor with IC50 of 62 nM.
  • Hepatology, 2013, 57(1):70-80
  • MOLECULAR ONCOLOGY, 2013, 7(6):1093-102
  • J Thorac Oncol, 2012, 7(7):1078-85
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.
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
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.
S8039 PU-H71 PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 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.
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
  • Acta Pharmacol Sin, 2013, 34(12):1545-53
S1163 AT13387 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
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
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
  • Biochem Pharmacol, 2012, 20(3):400-13
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, 2014, 10.1128/AAC.02576-14
S2685 KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 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
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
  • Antimicrob Agents Chemother, 2013, 57(2):1035-9