HSP (HSP90)

Choose Selective HSP (HSP90) Inhibitors

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Signaling Pathways

HSP (HSP90) Products

  • All (43)
  • HSP (HSP90) Inhibitors (31)
  • 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
E0249New Pseudolaric Acid A Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and anticancer activities.
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.
Biomedicines, 2022, 10(3)624
Cell Death Discov, 2022, 8(1):86
Cell Rep, 2021, 34(11):108870
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.
Blood Cancer J, 2022, 12(3):39
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Cell Mol Med, 2022, 10.1111/jcmm.17210
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.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Biomedicines, 2022, 10(3)624
SLAS Discov, 2022, 27(3):175-184
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.
Biomedicines, 2022, 10(3)624
Nat Commun, 2021, 12(1):5919
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.
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2021, S2451-9456(21)00221-X
Transl Res, 2021, 235:1-14
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.
SLAS Discov, 2022, 27(3):175-184
Front Oncol, 2021, 11:620907
SLAS Technol, 2019, 24(1):28-40
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.
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
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.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
Cell Chem Biol, 2021, S2451-9456(21)00221-X
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.
Chin Med J (Engl), 2022, 135(5):606-618
Shock, 2021, 55(1):74-82
Radiat Res, 2020, 193(2):119-129
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.
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
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).
S6193 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.
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2016, 23(6):716-26
Oncotarget, 2016, 7(31):49597-49610
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.
SLAS Discov, 2022, 27(3):175-184
J Exp Clin Cancer Res, 2021, 40(1):170
Immunity, 2020, 52(2):328-341
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
S7428 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.
SLAS Discov, 2022, 27(3):175-184
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.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
EMBO J, 2021, e106183
Oncogene, 2021, 10.1038/s41388-021-01914-2
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
S9806 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.
Blood Cancer J, 2022, 12(3):36
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
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.
Front Oncol, 2022, 12:842418
Bone, 2022, 154:116262
Biomedicines, 2021, 9(2)E96
S8305 TRC051384 TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
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
E0249New Pseudolaric Acid A Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and anticancer activities.
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.
Biomedicines, 2022, 10(3)624
Cell Death Discov, 2022, 8(1):86
Cell Rep, 2021, 34(11):108870
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.
Blood Cancer J, 2022, 12(3):39
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Cell Mol Med, 2022, 10.1111/jcmm.17210
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.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Biomedicines, 2022, 10(3)624
SLAS Discov, 2022, 27(3):175-184
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.
Biomedicines, 2022, 10(3)624
Nat Commun, 2021, 12(1):5919
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.
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2021, S2451-9456(21)00221-X
Transl Res, 2021, 235:1-14
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.
SLAS Discov, 2022, 27(3):175-184
Front Oncol, 2021, 11:620907
SLAS Technol, 2019, 24(1):28-40
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.
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
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.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
Cell Chem Biol, 2021, S2451-9456(21)00221-X
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.
Chin Med J (Engl), 2022, 135(5):606-618
Shock, 2021, 55(1):74-82
Radiat Res, 2020, 193(2):119-129
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.
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
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).
S6193 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.
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2016, 23(6):716-26
Oncotarget, 2016, 7(31):49597-49610
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.
SLAS Discov, 2022, 27(3):175-184
J Exp Clin Cancer Res, 2021, 40(1):170
Immunity, 2020, 52(2):328-341
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
S7428 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.
SLAS Discov, 2022, 27(3):175-184
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.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
EMBO J, 2021, e106183
Oncogene, 2021, 10.1038/s41388-021-01914-2
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
S9806 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.
Blood Cancer J, 2022, 12(3):36
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
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.
Front Oncol, 2022, 12:842418
Bone, 2022, 154:116262
Biomedicines, 2021, 9(2)E96
S8305 TRC051384 TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
E0249New Pseudolaric Acid A Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and 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