HSP (HSP90)
Inhibitory Selectivity
Isoform-specific Inhibitors
HSP (HSP90) Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1175 |
BIIB021BIIB021 (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. |
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| S1498 |
NVP-BEP800NVP-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. |
Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800). |
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| 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. |
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| 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.
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| 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.
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| E1208New |
NPX800NPX800 is a potent heat shock factor 1 (HSF1) inhibitor, which has the potential for cancer research. |
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| S2930 |
Pifithrin-μPifithrin-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. |
Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
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| S8039 |
Zelavespib (PU-H71)Zelavespib (PU-H71, NSC 750424) 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.
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| S8365 |
ApoptozoleApoptozole (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. |
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.
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| 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). KRIBB11 induces growth arrest and apoptosis. |
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| S9806 |
DTHIBDTHIB (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. |
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| S7428 |
RocaglamideRocaglamide (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. |
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| 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.
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| 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). |
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| S7340 |
CH5138303CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM. |
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| S7459 |
VER-50589VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β. |
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| S6193 |
YUM70YUM70 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. |
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| S7751 |
VER155008VER155008 (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. |
(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). |
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| S6721 |
JG98JG-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. |
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| 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. |
Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.
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| 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. |
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| S0279 |
DimethylenastronDimethylenastron 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. |
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| S0294 |
HSF1AHSF1A 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. |
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| S6568 |
ML346ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. |
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| S8305 |
TRC051384TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
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| S8299 |
HA15HA15 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. |
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 |
|---|---|---|---|
| S1175 |
BIIB021BIIB021 (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. |
|
|
| S1498 |
NVP-BEP800NVP-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. |
Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800). |
|
| 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.
|
|
| 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.
|
|
| E1208New |
NPX800NPX800 is a potent heat shock factor 1 (HSF1) inhibitor, which has the potential for cancer research. |
||
| S2930 |
Pifithrin-μPifithrin-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. |
Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
|
|
| S8039 |
Zelavespib (PU-H71)Zelavespib (PU-H71, NSC 750424) 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.
|
|
| S8365 |
ApoptozoleApoptozole (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. |
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). KRIBB11 induces growth arrest and apoptosis. |
||
| S9806 |
DTHIBDTHIB (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. |
||
| S7428 |
RocaglamideRocaglamide (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. |
||
| 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.
|
|
| 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). |
||
| 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. |
||
| S6193 |
YUM70YUM70 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. |
||
| S7751 |
VER155008VER155008 (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. |
(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). |
|
| S6721 |
JG98JG-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. |
Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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 |
DimethylenastronDimethylenastron 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 |
HSF1AHSF1A 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 |
ML346ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8305 |
TRC051384TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
||
| S8299 |
HA15HA15 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. |
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.
|
