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HSP (HSP90) Products

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HSP (HSP90) Inhibitors (31)
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New HSP (HSP90) Products

Catalog No.	Product Name	Information	Product Use Citations
E0249^New	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 K_i 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 K_a 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 K_d 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 K_d 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 K_d 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).
E0362^New	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
E0249^New	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 K_i 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 K_a 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 K_d 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 K_d 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 K_d 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).
E0362^New	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
E0249^New	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.
E0362^New	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.