HSP (HSP90)

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HSP (HSP90)シグナル伝達経路

HSP (HSP90)製品

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  • HSP (HSP90)阻害剤 (31)
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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 Death Dis, 2024, 15(1):35
Sci Adv, 2024, 10(8):eadk3663
Signal Transduct Target Ther, 2023, 8(1):229
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.
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis).
Cell Death Dis, 2024, 15(2):149
J Exp Clin Cancer Res, 2023, 42(1):251
Cell Chem Biol, 2023, 30(9):1064-1075.e8
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.
Sci Adv, 2024, 10(8):eadk3663
Nat Commun, 2023, 14(1):1516
Mol Cell, 2023, S1097-2765(23)00377-5
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.
Nature, 2024, 626(8000):874-880
Int J Mol Sci, 2023, 24(15)12476
Virus Res, 2023, 329:199103
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Nat Commun, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):3469
S7751 VER155008 VER155008 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.
Signal Transduct Target Ther, 2023, 8(1):229
Mol Cell, 2023, 83(15):2810-2828.e6
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
S3604 Triptolide Triptolide 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.
Clin Transl Med, 2024, 14(2):e1567
Acta Pharmacol Sin, 2024, 10.1038/s41401-023-01219-y
Cancer Sci, 2024, 10.1111/cas.16076
S2713 Geldanamycin Geldanamycin 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.
Int J Mol Sci, 2023, 24(18)13830
ACS Cent Sci, 2022, 8(5):636-655
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
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.
Cell Rep, 2022, 41(4):111546
SLAS Discov, 2022, 27(3):175-184
Front Oncol, 2021, 11:804412
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.
Nature Communications, 2023, 1221-2023)
Cancers (Basel), 2023, 15(17)4239
Cancers (Basel), 2023, 15(17)4239
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.
iScience, 2023, 26(7):107090
Heliyon, 2023, 9(3):e14169
FEBS Open Bio, 2023, none
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
S1972 Tamoxifen Citrate Tamoxifen Citrate 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.
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
NAR Cancer, 2023, 5(2):zcad023
S2639 SNX-2112 SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.
NPJ Breast Cancer, 2022, 8(1):96
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2021, S2451-9456(21)00221-X
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.
Nat Commun, 2023, 14(1):6473
Nat Commun, 2023, 14(1):6473
J Biol Chem, 2023, 299(6):104710
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.
Clin Transl Med, 2024, 14(2):e1567
iScience, 2023, 26(1):105743
Front Oncol, 2022, 12:842418
S8039 Zelavespib (PU-H71) Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
Int J Mol Sci, 2023, 24(14)11585
EJNMMI Radiopharm Chem, 2023, 8(1):2
ACS Cent Sci, 2022, 8(5):636-655
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.
Virus Res, 2023, 329:199103
Nature, 2022, 607(7917):149-155
EMBO Mol Med, 2022, 14(12):e15677
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
Mol Cancer, 2020, 19(1):112
S8365 Apoptozole Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70. It induces caspase-dependent apoptosis.
Nutrients, 2023, 15(4)992
J Virol, 2023, 97(4):e0012823
Int J Mol Sci, 2022, 23(23)15229
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
Sci Adv, 2023, 9(35):eade7486
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2016, 23(6):716-26
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
S7750 KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
Parasit Vectors, 2023, 16(1):168
Biosci Rep, 2020, 40(3)
Br J Haematol, 2013, 161(5):667-76
S5006 Teprenone Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis.
Inflammopharmacology, 2023, 31(3):1319-1327
Antioxidants -Basel, 2022, 11-91741
Front Endocrinol (Lausanne), 2021, 12:743202
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
Front Cell Dev Biol, 2021, 9:796974
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
S7459 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
Antiviral Res, 2023, 211:105553
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2014, 8(2):e2699
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.
Elife, 2023, 12e69521
Blood Adv, 2023, 7(12):2926-2937
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
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).
Hum Exp Toxicol, 2023, 42:9603271231165678
Cancer Res, 2022, CAN-21-3819
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.
FEBS Open Bio, 2023, none
Cell Rep, 2022, 40(13):111428
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
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.
EMBO Rep, 2023, e57234.
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.
Cancer Sci, 2023, 114(11):4388-4400.
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.
S6568 ML346 ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases.
E0362 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.

E0249 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.
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
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.Although YUM70 inhibits GRP78 enzymatic activity, it increases the expression of GRP78 by increasing the chaperone translation mechanism.
E0701 Cucurbitacin D Cucurbitacin D is an active component in Cucurbita texana, disrupts maturation of HSP90 and interactions between Hsp90 and two co-chaperones, Cdc37 and p23.
E1208 NPX800 NPX800 is a potent heat shock factor 1 (HSF1) inhibitor, which has the potential for cancer research.
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 Death Dis, 2024, 15(1):35
Sci Adv, 2024, 10(8):eadk3663
Signal Transduct Target Ther, 2023, 8(1):229
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.
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
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.
Sci Adv, 2024, 10(8):eadk3663
Nat Commun, 2023, 14(1):1516
Mol Cell, 2023, S1097-2765(23)00377-5
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.
Nature, 2024, 626(8000):874-880
Int J Mol Sci, 2023, 24(15)12476
Virus Res, 2023, 329:199103
S7751 VER155008 VER155008 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.
Signal Transduct Target Ther, 2023, 8(1):229
Mol Cell, 2023, 83(15):2810-2828.e6
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
S3604 Triptolide Triptolide 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.
Clin Transl Med, 2024, 14(2):e1567
Acta Pharmacol Sin, 2024, 10.1038/s41401-023-01219-y
Cancer Sci, 2024, 10.1111/cas.16076
S2713 Geldanamycin Geldanamycin 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.
Int J Mol Sci, 2023, 24(18)13830
ACS Cent Sci, 2022, 8(5):636-655
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
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.
Cell Rep, 2022, 41(4):111546
SLAS Discov, 2022, 27(3):175-184
Front Oncol, 2021, 11:804412
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.
Nature Communications, 2023, 1221-2023)
Cancers (Basel), 2023, 15(17)4239
Cancers (Basel), 2023, 15(17)4239
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.
iScience, 2023, 26(7):107090
Heliyon, 2023, 9(3):e14169
FEBS Open Bio, 2023, none
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 SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.
NPJ Breast Cancer, 2022, 8(1):96
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2021, S2451-9456(21)00221-X
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.
Nat Commun, 2023, 14(1):6473
Nat Commun, 2023, 14(1):6473
J Biol Chem, 2023, 299(6):104710
S8039 Zelavespib (PU-H71) Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
Int J Mol Sci, 2023, 24(14)11585
EJNMMI Radiopharm Chem, 2023, 8(1):2
ACS Cent Sci, 2022, 8(5):636-655
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.
Virus Res, 2023, 329:199103
Nature, 2022, 607(7917):149-155
EMBO Mol Med, 2022, 14(12):e15677
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
Mol Cancer, 2020, 19(1):112
S8365 Apoptozole Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70. It induces caspase-dependent apoptosis.
Nutrients, 2023, 15(4)992
J Virol, 2023, 97(4):e0012823
Int J Mol Sci, 2022, 23(23)15229
S7122 XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.
Sci Adv, 2023, 9(35):eade7486
SLAS Discov, 2022, 27(3):175-184
Cell Chem Biol, 2016, 23(6):716-26
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
S7750 KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
Parasit Vectors, 2023, 16(1):168
Biosci Rep, 2020, 40(3)
Br J Haematol, 2013, 161(5):667-76
S7459 VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
Antiviral Res, 2023, 211:105553
Cell Chem Biol, 2021, S2451-9456(21)00221-X
PLoS Negl Trop Dis, 2014, 8(2):e2699
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.
Elife, 2023, 12e69521
Blood Adv, 2023, 7(12):2926-2937
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
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).
Hum Exp Toxicol, 2023, 42:9603271231165678
Cancer Res, 2022, CAN-21-3819
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.
FEBS Open Bio, 2023, none
Cell Rep, 2022, 40(13):111428
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
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.
Cancer Sci, 2023, 114(11):4388-4400.
E0249 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.
S7340 CH5138303 CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
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.Although YUM70 inhibits GRP78 enzymatic activity, it increases the expression of GRP78 by increasing the chaperone translation mechanism.
E1208 NPX800 NPX800 is a potent heat shock factor 1 (HSF1) inhibitor, which has the potential for cancer research.
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Nat Commun, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):3469
S1972 Tamoxifen Citrate Tamoxifen Citrate 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.
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
NAR Cancer, 2023, 5(2):zcad023
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.
EMBO Rep, 2023, e57234.
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.
S6568 ML346 ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases.
E0362 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.

S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis).
Cell Death Dis, 2024, 15(2):149
J Exp Clin Cancer Res, 2023, 42(1):251
Cell Chem Biol, 2023, 30(9):1064-1075.e8
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.
Clin Transl Med, 2024, 14(2):e1567
iScience, 2023, 26(1):105743
Front Oncol, 2022, 12:842418
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
Front Cell Dev Biol, 2021, 9:796974
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
E0701 Cucurbitacin D Cucurbitacin D is an active component in Cucurbita texana, disrupts maturation of HSP90 and interactions between Hsp90 and two co-chaperones, Cdc37 and p23.

HSP (HSP90)阻害剤の選択性比較

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