HSP (e.g. HSP90)

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

HSP (e.g. HSP90) Products

All (24) HSP (e.g. HSP90) Inhibitors (21) HSP (e.g. HSP90) Modulators (3)

Catalog No.	Information	Product Use Citations	Product Validations
S1141	Tanespimycin (17-AAG) Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Phase 2.	Br J Pharmacol, 2017, 174(5):409-423 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7 Oncotarget, 2015, 51: S659-S660	SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
S1069	Luminespib (AUY-922, NVP-AUY922) Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2.	Sci Rep, 2017, 7(1):201 Cancer Lett, 2016, 372(1):75-81 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7
S1142	Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.	Experimental Cell Research, 2017, 353(1):46-53 Cell Death Dis, 2016, 7(6):e2290 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7
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.	Mol Cancer Res, 2018, 10.1158/1541-7786 Nature, 2017, 10.1038/nature21064 Cell, 2017, 168(5):856-866	Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.
S1175	BIIB021 BIIB021 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.	Endocrinology, 2018, 159(2):907-930 Cell, 2017, 168(5):856-866 Biomed Pharmacother, 2016, 83:22-32
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, 2017, 168(5):856-866 PLoS One, 2017, 12(5):e0177878 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7	IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A) inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and analyzed by GraphPad.Prism.
S1498	NVP-BEP800 NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1.	Mol Cancer, 2017, 16(1):72 Cell Death Dis, 2016, 7:e2051 PLoS Negl Trop Dis, 2015, 8(2):e2699	Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).
S2713	Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.	Radiat Res, 2018, 189(5):519-528 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7 J Antimicrob Chemother, 2015, 10.1093/jac/dku549	Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
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.	Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7 Immunopharmacol Immunotoxicol, 2015, 8:1-10 PLoS Negl Trop Dis, 2014, 8(2):e2699
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.	Endocrine, 2016, 51(2):274-82 Antimicrob Agents Chemother, 2014, 58(7):4138-44 J Biol Chem, 2013, 288(23):16308-20	Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
S2685	KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.
S7122	XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.	Clin Cancer Res, 2012, 18(9):2502-14	B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.
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.	Theranostics, 2019, 9(2):554-572 Acta Histochem, 2015, 117(8):705-11	(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
S8039	PU-H71 PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.	Cell, 2017, 168(5):856-866 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7	Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.
S8365	Apoptozole Apoptozole is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis.	Platelets, 2018, 29(6):610-621	Representative images of platelets preincubated with FITC-conjugated CD41 before treated with negative control, pitstop 2, dynasore, A23, or apoptozole spreading on immobilized Fg for 10, 30, and 60 minutes, respectively. Images were taken under oil immersion with magnification × 100. Scale bar, 5 μm.
S8402	KRIBB11 KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1).
S7750	KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.	Br J Haematol, 2013, 161(5):667-76 Oncol Rep, 2012, 28(6):1953-8	Western blots of lysates from BaF3 JAK2 V617F cells.
S7458	VER-49009 VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
S7340	CH5138303 CH5138303 is an orally available Hsp90 inhibitor with K_d of 0.48 nM.
S7459	VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.	PLoS Negl Trop Dis, 2014, 8(2):e2699
S7751	VER155008 VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.	Cancer Sci, 2018, 109(2):373-383 Antiviral Res, 2018, 150:39-46 Cell Signal, 2017, 30:130-141	(D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM).
S1052	Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.	Osteoporos Int, 2018, 29(8):1917-1926 Oncol Rep, 2018, 40(2):635-646 Cell, 2017, 168(1-2):86-100
S8305	TRC051384 TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.
S8299	HA15 HA15 is a molecule that targets specifically BiP/GRP78/HSPA5. HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.	Br J Cancer, 2018, 119(1):65-75	SP cells in inhibitor-treated, shRNA-transduced HCC1937 cells analyzed by flow cytometry using Hoechst 33342 dye. Data are shown as mean±SD. **P<.0001, P<.001, P<.01, P<.05.

Catalog No.	Information	Product Use Citations	Product Validations
S1141	Tanespimycin (17-AAG) Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Phase 2.	Br J Pharmacol, 2017, 174(5):409-423 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7 Oncotarget, 2015, 51: S659-S660	SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
S1069	Luminespib (AUY-922, NVP-AUY922) Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2.	Sci Rep, 2017, 7(1):201 Cancer Lett, 2016, 372(1):75-81 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7
S1142	Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.	Experimental Cell Research, 2017, 353(1):46-53 Cell Death Dis, 2016, 7(6):e2290 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7
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.	Mol Cancer Res, 2018, 10.1158/1541-7786 Nature, 2017, 10.1038/nature21064 Cell, 2017, 168(5):856-866	Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.
S1175	BIIB021 BIIB021 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.	Endocrinology, 2018, 159(2):907-930 Cell, 2017, 168(5):856-866 Biomed Pharmacother, 2016, 83:22-32
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, 2017, 168(5):856-866 PLoS One, 2017, 12(5):e0177878 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7	IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A) inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and analyzed by GraphPad.Prism.
S1498	NVP-BEP800 NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1.	Mol Cancer, 2017, 16(1):72 Cell Death Dis, 2016, 7:e2051 PLoS Negl Trop Dis, 2015, 8(2):e2699	Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).
S2713	Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.	Radiat Res, 2018, 189(5):519-528 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7 J Antimicrob Chemother, 2015, 10.1093/jac/dku549	Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
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.	Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7 Immunopharmacol Immunotoxicol, 2015, 8:1-10 PLoS Negl Trop Dis, 2014, 8(2):e2699
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.	Endocrine, 2016, 51(2):274-82 Antimicrob Agents Chemother, 2014, 58(7):4138-44 J Biol Chem, 2013, 288(23):16308-20	Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
S2685	KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.
S7122	XL888 XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1.	Clin Cancer Res, 2012, 18(9):2502-14	B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.
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.	Theranostics, 2019, 9(2):554-572 Acta Histochem, 2015, 117(8):705-11	(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
S8039	PU-H71 PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.	Cell, 2017, 168(5):856-866 Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7	Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.
S8365	Apoptozole Apoptozole is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis.	Platelets, 2018, 29(6):610-621	Representative images of platelets preincubated with FITC-conjugated CD41 before treated with negative control, pitstop 2, dynasore, A23, or apoptozole spreading on immobilized Fg for 10, 30, and 60 minutes, respectively. Images were taken under oil immersion with magnification × 100. Scale bar, 5 μm.
S8402	KRIBB11 KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1).
S7750	KNK437 KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.	Br J Haematol, 2013, 161(5):667-76 Oncol Rep, 2012, 28(6):1953-8	Western blots of lysates from BaF3 JAK2 V617F cells.
S7458	VER-49009 VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
S7340	CH5138303 CH5138303 is an orally available Hsp90 inhibitor with K_d of 0.48 nM.
S7459	VER-50589 VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.	PLoS Negl Trop Dis, 2014, 8(2):e2699
S7751	VER155008 VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.	Cancer Sci, 2018, 109(2):373-383 Antiviral Res, 2018, 150:39-46 Cell Signal, 2017, 30:130-141	(D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM).

Catalog No.	Information	Product Use Citations	Product Validations
S1052	Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.	Osteoporos Int, 2018, 29(8):1917-1926 Oncol Rep, 2018, 40(2):635-646 Cell, 2017, 168(1-2):86-100
S8305	TRC051384 TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent.
S8299	HA15 HA15 is a molecule that targets specifically BiP/GRP78/HSPA5. HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.	Br J Cancer, 2018, 119(1):65-75	SP cells in inhibitor-treated, shRNA-transduced HCC1937 cells analyzed by flow cytometry using Hoechst 33342 dye. Data are shown as mean±SD. **P<.0001, P<.001, P<.01, P<.05.

Catalog No.

Information

Product Use Citations

Product Validations

S1052

Elesclomol (STA-4783)

Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.

Osteoporos Int, 2018, 29(8):1917-1926

Oncol Rep, 2018, 40(2):635-646

Cell, 2017, 168(1-2):86-100

S8305

TRC051384

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

S8299

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

Br J Cancer, 2018, 119(1):65-75