HSP (e.g. HSP90)
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
HSP (e.g. HSP90) Products
| 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. |
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 (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. |
|
|
| S1142 |
Alvespimycin (17-DMAG) HClAlvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2. |
|
|
| 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. |
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.
|
|
| S6721New |
JG98JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. |
||
| S7716New |
TAS-116TAS-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). |
||
| S1175 |
BIIB021BIIB021 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. |
|
|
| 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. |
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-BEP800NVP-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. |
Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800). |
|
| S2713 |
GeldanamycinGeldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. |
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 Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG. |
|
|
| 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. |
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-2478KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. |
||
| S7122 |
XL888XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
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-E973NMS-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. |
(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-H71PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
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.
|
|
| S5369 |
EthoxyquinEthoxyquin 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). |
||
| S8365 |
ApoptozoleApoptozole 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. |
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 |
KRIBB11KRIBB11 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 |
KNK437KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40. |
Western blots of lysates from BaF3 JAK2 V617F cells.
|
|
| S7458 |
VER-49009VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
||
| S7340 |
CH5138303CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM. |
||
| S7459 |
VER-50589VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β. |
||
| S7751 |
VER155008VER-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. |
(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). |
|
| S6568New |
ML346ML346 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. |
|
|
| S8305 |
TRC051384TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
||
| S8299 |
HA15HA15 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. |
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.
|
|
| S5006 |
TeprenoneTeprenone, 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. |
| 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. |
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 (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. |
|
|
| S1142 |
Alvespimycin (17-DMAG) HClAlvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2. |
|
|
| 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. |
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.
|
|
| S6721New |
JG98JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. |
||
| S7716New |
TAS-116TAS-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). |
||
| S1175 |
BIIB021BIIB021 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. |
|
|
| 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. |
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-BEP800NVP-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. |
Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800). |
|
| S2713 |
GeldanamycinGeldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. |
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 Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG. |
|
|
| 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. |
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-2478KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. |
||
| S7122 |
XL888XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
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-E973NMS-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. |
(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-H71PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
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.
|
|
| S5369 |
EthoxyquinEthoxyquin 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). |
||
| S8365 |
ApoptozoleApoptozole 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. |
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 |
KRIBB11KRIBB11 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 |
KNK437KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40. |
Western blots of lysates from BaF3 JAK2 V617F cells.
|
|
| S7458 |
VER-49009VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
||
| S7340 |
CH5138303CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM. |
||
| S7459 |
VER-50589VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β. |
||
| S7751 |
VER155008VER-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. |
(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 |
|---|---|---|---|
| S6568New |
ML346ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. |
| 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. |
|
|
| S8305 |
TRC051384TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
||
| S8299 |
HA15HA15 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. |
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 |
|---|---|---|---|
| S5006 |
TeprenoneTeprenone, 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. |
