HSP (e.g. HSP90)

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1141 Tanespimycin (17-AAG) <1 mg/mL 100 mg/mL 5 mg/mL
S1069 Luminespib (AUY-922, NVP-AUY922) <1 mg/mL 93 mg/mL 31 mg/mL
S1142 Alvespimycin (17-DMAG) 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
S8305 TRC051384 <1 mg/mL 93 mg/mL 5 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
S1498 NVP-BEP800 <1 mg/mL <1 mg/mL 15 mg/mL
S2713 Geldanamycin <1 mg/mL 36 mg/mL <1 mg/mL
S2639 SNX-2112 (PF-04928473) <1 mg/mL 93 mg/mL 1 mg/mL
S2656 PF-04929113 (SNX-5422) <1 mg/mL 104 mg/mL 5 mg/mL
S2685 KW-2478 <1 mg/mL 115 mg/mL 3 mg/mL
S7122 XL888 <1 mg/mL 100 mg/mL <1 mg/mL
S7282 NMS-E973 <1 mg/mL 90 mg/mL <1 mg/mL
S8039 PU-H71 34 mg/mL 100 mg/mL 100 mg/mL
S8365 Apoptozole <1 mg/mL 100 mg/mL 25 mg/mL
S8402 KRIBB11 <1 mg/mL 3 mg/mL <1 mg/mL
S7750 KNK437 <1 mg/mL 15 mg/mL <1 mg/mL
S7458 VER-49009 <1 mg/mL 77 mg/mL <1 mg/mL
S8299 HA15 <1 mg/mL 93 mg/mL 45 mg/mL
S7340 CH5138303 <1 mg/mL 83 mg/mL <1 mg/mL
S7459 VER-50589 <1 mg/mL 77 mg/mL 77 mg/mL
S7751 VER155008 <1 mg/mL 100 mg/mL <1 mg/mL
S7097 HSP990 (NVP-HSP990) <1 mg/mL 75 mg/mL <1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1141

Tanespimycin (17-AAG)

Tanespimycin (17-AAG) 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.

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-molecule HSP90 ligand. Phase 2.

S1142

Alvespimycin (17-DMAG) HCl

Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

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.

S8305New

TRC051384

TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.

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.

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.

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.

S2713

Geldanamycin

Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

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.

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.

S2685

KW-2478

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.

S7122

XL888

XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.

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.

S8039

PU-H71

PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

S8365

Apoptozole

Apoptozole is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis.

S8402

KRIBB11

KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1).

S7750

KNK437

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

S7458

VER-49009

VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.

S8299

HA15

HA15 is a molecule that targets specifically BiP/GRP78/HSPA5. HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

S7340

CH5138303

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

S7459

VER-50589

VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.

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.

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.

Tags: HSP90 inhibition | HSP90 activity | HSP90 inhibitor cancer | HSP90 activation | HSP90 phosphorylation | HSP90 inhibitors in clinical trials | HSP70 assay | HSP70 phosphorylation | HSP90 inhibitor review