HSP (HSP90)

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HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Signaling Pathways

HSP (HSP90) Products

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  • HSP (HSP90) Inhibitors (30)
  • HSP (HSP90) Antibodies (2)
  • HSP (HSP90) Activators (6)
  • HSP (HSP90) Modulators (3)
  • New HSP (HSP90) Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Cell Rep, 2021, 34(11):108870
Haematologica, 2021, 10.3324/haematol.2021.278743
Cancers (Basel), 2021, 13(15)3850
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.
Cell Stem Cell, 2021, S1934-5909(21)00294-0
Mol Cell, 2021, 81(6):1170-1186.e10
EMBO Rep, 2021, e51740
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. Phase 2.
Sci Adv, 2021, 7(7)eabd2645
Nat Commun, 2021, 12(1):7204
Cancer Sci, 2021, 10.1111/cas.15204
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.
Nat Commun, 2021, 12(1):5919
Cell Death Dis, 2021, 12(1):126
Cell Death Dis, 2021, 12(1):126
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.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
Transl Res, 2021, 235:1-14
Front Oncol, 2021, 11:642603
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.
Front Oncol, 2021, 11:620907
SLAS Technol, 2019, 24(1):28-40
ACS Chem Neurosci, 2019, 10(6):2890-2902
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.
Blood Cancer J, 2021, 11(3):61
Cell Death Dis, 2021, 12(1):114
Cell Death Dis, 2021, 12(1):114
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.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
Onco Targets Ther, 2020, 13:7907-7919
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.
ACS Chem Neurosci, 2019, 10(6):2890-2902
Endocrine, 2016, 51(2):274-82
Antimicrob Agents Chemother, 2014, 58(7):4138-44
S2685 KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.
Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
S2713 Geldanamycin (NSC 122750) Geldanamycin (NSC 122750) 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.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
J Virol, 2021, JVI0059421
Int J Pharm, 2021, 610:121272
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Shock, 2021, 55(1):74-82
Radiat Res, 2020, 193(2):119-129
Clin Transl Med, 2020, 10.1002/ctm2.41
S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00657-w
S5369 Ethoxyquin Ethoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative. Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).
S6193New YUM70 YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.
S6721 JG98 JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity.
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.
Mol Cancer Res, 2020, 18(7):1004-1017
Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669
Theranostics, 2020, 10(18):8415-8429
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
Cell Chem Biol, 2016, 23(6):716-26
Oncotarget, 2016, 7(31):49597-49610
Clin Cancer Res, 2012, 18(9):2502-14
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.
J Exp Clin Cancer Res, 2021, 40(1):170
Immunity, 2020, 52(2):328-341
Mol Cancer, 2020, 19(1):112
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
S7428New Rocaglamide Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity.
S7458 VER-49009 VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
S7459 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2014, 8(2):e2699
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).
S7750 KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
Biosci Rep, 2020, 40(3)
Br J Haematol, 2013, 161(5):667-76
Oncol Rep, 2012, 28(6):1953-8
S7751 VER155008 VER155008 (C07) 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 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
EMBO J, 2021, e106183
Oncogene, 2021, 10.1038/s41388-021-01914-2
Eur J Med Chem, 2021, 220:113452
S8039 Zelavespib (PU-H71) Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
Nat Cancer, 2021, 2(6):598-610
Cancers (Basel), 2020, 7;12(4)
Mol Cell Biol, 2020,
S8365 Apoptozole Apoptozole (Apoptosis Activator VII) 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.
Nat Commun, 2018, 9(1):4700
Platelets, 2018, 29(6):610-621
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). KRIBB11 induces growth arrest and apoptosis.
Cell Metab, 2021, S1550-4131(21)00183-2
Br J Pharmacol, 2021, 178(5):1182-1199
Cancers (Basel), 2021, 13(12)2987
S9806New DTHIB DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
A5110 Hsc70 Rabbit Recombinant mAb Hsc70 Rabbit Recombinant mAb detects endogenous levels of total Hsc70.
A5260 Phospho-HSF1(S326) Rabbit Recombinant mAb Phospho-HSF1(S326) Rabbit Recombinant mAb detects endogenous level of total phospho-HSF1(S326).
E0362New BiP Inducer X (BIX)

BiP Inducer X (BIX) is a selective GRP78 (BiP, HSPA5) inducer. BIX induces BiP only, in a dose-dependent manner, without induction of other molecules involved in the ER stress response.

S0279 Dimethylenastron Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.
S0294 HSF1A HSF1A is a cell-permeable heat shock transcription factor 1 (HSF1) activator. HSF1A protects cells from stress-induced apoptosis, binds TRiC subunits and inhibits TRiC activity without perturbation of ATP hydrolysis.
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S1972 Tamoxifen (ICI 46474) Citrate Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S6568 ML346 ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases.
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
J Exp Clin Cancer Res, 2021, 40(1):228
Mol Oncol, 2021, 10.1002/1878-0261.13079
Nat Commun, 2020, 15;11(1):2423
S8299 HA15 HA15 is a molecule that targets specifically HSPA5 (Heat shock 70kDa protein 5) also known as BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.
Bone, 2022, 154:116262
Biomedicines, 2021, 9(2)E96
ACS Appl Mater Interfaces, 2020, 12(1):352-360
S8305 TRC051384 TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
S5006 Teprenone Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis. Teprenone(Geranylgeranylacetone) is an inducer of heat shock proteins (HSPs) expression.
Front Endocrinol (Lausanne), 2021, 12:743202
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.
Cell Rep, 2021, 34(11):108870
Haematologica, 2021, 10.3324/haematol.2021.278743
Cancers (Basel), 2021, 13(15)3850
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.
Cell Stem Cell, 2021, S1934-5909(21)00294-0
Mol Cell, 2021, 81(6):1170-1186.e10
EMBO Rep, 2021, e51740
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. Phase 2.
Sci Adv, 2021, 7(7)eabd2645
Nat Commun, 2021, 12(1):7204
Cancer Sci, 2021, 10.1111/cas.15204
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.
Nat Commun, 2021, 12(1):5919
Cell Death Dis, 2021, 12(1):126
Cell Death Dis, 2021, 12(1):126
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.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
Transl Res, 2021, 235:1-14
Front Oncol, 2021, 11:642603
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.
Front Oncol, 2021, 11:620907
SLAS Technol, 2019, 24(1):28-40
ACS Chem Neurosci, 2019, 10(6):2890-2902
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.
Blood Cancer J, 2021, 11(3):61
Cell Death Dis, 2021, 12(1):114
Cell Death Dis, 2021, 12(1):114
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.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
Onco Targets Ther, 2020, 13:7907-7919
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.
ACS Chem Neurosci, 2019, 10(6):2890-2902
Endocrine, 2016, 51(2):274-82
Antimicrob Agents Chemother, 2014, 58(7):4138-44
S2685 KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.
Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
S2713 Geldanamycin (NSC 122750) Geldanamycin (NSC 122750) 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.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
J Virol, 2021, JVI0059421
Int J Pharm, 2021, 610:121272
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Shock, 2021, 55(1):74-82
Radiat Res, 2020, 193(2):119-129
Clin Transl Med, 2020, 10.1002/ctm2.41
S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00657-w
S5369 Ethoxyquin Ethoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative. Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).
S6193New YUM70 YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.
S6721 JG98 JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity.
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.
Mol Cancer Res, 2020, 18(7):1004-1017
Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669
Theranostics, 2020, 10(18):8415-8429
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
Cell Chem Biol, 2016, 23(6):716-26
Oncotarget, 2016, 7(31):49597-49610
Clin Cancer Res, 2012, 18(9):2502-14
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.
J Exp Clin Cancer Res, 2021, 40(1):170
Immunity, 2020, 52(2):328-341
Mol Cancer, 2020, 19(1):112
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
S7428New Rocaglamide Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity.
S7458 VER-49009 VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
S7459 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2014, 8(2):e2699
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).
S7750 KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
Biosci Rep, 2020, 40(3)
Br J Haematol, 2013, 161(5):667-76
Oncol Rep, 2012, 28(6):1953-8
S7751 VER155008 VER155008 (C07) 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 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
EMBO J, 2021, e106183
Oncogene, 2021, 10.1038/s41388-021-01914-2
Eur J Med Chem, 2021, 220:113452
S8039 Zelavespib (PU-H71) Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
Nat Cancer, 2021, 2(6):598-610
Cancers (Basel), 2020, 7;12(4)
Mol Cell Biol, 2020,
S8365 Apoptozole Apoptozole (Apoptosis Activator VII) 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.
Nat Commun, 2018, 9(1):4700
Platelets, 2018, 29(6):610-621
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). KRIBB11 induces growth arrest and apoptosis.
Cell Metab, 2021, S1550-4131(21)00183-2
Br J Pharmacol, 2021, 178(5):1182-1199
Cancers (Basel), 2021, 13(12)2987
S9806New DTHIB DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
A5110 Hsc70 Rabbit Recombinant mAb Hsc70 Rabbit Recombinant mAb detects endogenous levels of total Hsc70.
A5260 Phospho-HSF1(S326) Rabbit Recombinant mAb Phospho-HSF1(S326) Rabbit Recombinant mAb detects endogenous level of total phospho-HSF1(S326).
E0362New BiP Inducer X (BIX)

BiP Inducer X (BIX) is a selective GRP78 (BiP, HSPA5) inducer. BIX induces BiP only, in a dose-dependent manner, without induction of other molecules involved in the ER stress response.

S0279 Dimethylenastron Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.
S0294 HSF1A HSF1A is a cell-permeable heat shock transcription factor 1 (HSF1) activator. HSF1A protects cells from stress-induced apoptosis, binds TRiC subunits and inhibits TRiC activity without perturbation of ATP hydrolysis.
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S1972 Tamoxifen (ICI 46474) Citrate Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S6568 ML346 ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases.
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
J Exp Clin Cancer Res, 2021, 40(1):228
Mol Oncol, 2021, 10.1002/1878-0261.13079
Nat Commun, 2020, 15;11(1):2423
S8299 HA15 HA15 is a molecule that targets specifically HSPA5 (Heat shock 70kDa protein 5) also known as BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.
Bone, 2022, 154:116262
Biomedicines, 2021, 9(2)E96
ACS Appl Mater Interfaces, 2020, 12(1):352-360
S8305 TRC051384 TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
S6193New YUM70 YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.
S7428New Rocaglamide Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity.
S9806New DTHIB DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
E0362New BiP Inducer X (BIX)

BiP Inducer X (BIX) is a selective GRP78 (BiP, HSPA5) inducer. BIX induces BiP only, in a dose-dependent manner, without induction of other molecules involved in the ER stress response.

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