HSP (HSP90)

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1141 Tanespimycin (17-AAG) <1 mg/mL 100 mg/mL '5 mg/mL
S1069 Luminespib (NVP-AUY922) <1 mg/mL 93 mg/mL ''31 mg/mL
S1142 Alvespimycin (17-DMAG) HCl <1 mg/mL 131 mg/mL '<1 mg/mL
S1159 Ganetespib (STA-9090) <1 mg/mL 40 mg/mL '<1 mg/mL
S0279 Dimethylenastron <1 mg/mL 60 mg/mL '''''1.5 mg/mL
S6721 JG98 <1 mg/mL 8 mg/mL '<1 mg/mL
S1175 BIIB021 <1 mg/mL 64 mg/mL 2 mg/mL
S1163 Onalespib (AT13387) <1 mg/mL 25 mg/mL <1 mg/mL
S1498 NVP-BEP800 <1 mg/mL <1 mg/mL '15 mg/mL
S2713 Geldanamycin <1 mg/mL 36 mg/mL '<1 mg/mL
S2639 SNX-2112 (PF-04928473) <1 mg/mL 93 mg/mL 1 mg/mL
S2656 PF-04929113 (SNX-5422) <1 mg/mL 104 mg/mL 5 mg/mL
S2685 KW-2478 <1 mg/mL 115 mg/mL 3 mg/mL
S7122 XL888 <1 mg/mL 100 mg/mL <1 mg/mL
S7282 NMS-E973 <1 mg/mL 90 mg/mL <1 mg/mL
S8039 PU-H71 34 mg/mL 100 mg/mL 100 mg/mL
S8365 Apoptozole <1 mg/mL 100 mg/mL '25 mg/mL
S8402 KRIBB11 <1 mg/mL 3 mg/mL ''<1 mg/mL
S7750 KNK437 <1 mg/mL 15 mg/mL <1 mg/mL
S7458 VER-49009 <1 mg/mL 77 mg/mL <1 mg/mL
S7340 CH5138303 <1 mg/mL 83 mg/mL <1 mg/mL
S7459 VER-50589 <1 mg/mL 77 mg/mL 77 mg/mL
S7751 VER155008 <1 mg/mL 100 mg/mL '<1 mg/mL
S0294 HSF1A <1 mg/mL 82 mg/mL '''20 mg/mL
S6568 ML346 <1 mg/mL 4 mg/mL <1 mg/mL
S1972 Tamoxifen Citrate <1 mg/mL 100 mg/mL '100 mg/mL
S1238 Tamoxifen <1 mg/mL 74 mg/mL ''74 mg/mL
S1052 Elesclomol (STA-4783) <1 mg/mL 80 mg/mL <1 mg/mL
S8305 TRC051384 <1 mg/mL 93 mg/mL 5 mg/mL
S8299 HA15 <1 mg/mL 93 mg/mL 45 mg/mL
S5006 Teprenone -1 mg/mL 66 mg/mL '-1 mg/mL

亜型選択性的な製品

HSP (HSP90)製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 2.

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. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.

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.

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.

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.

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.

S7716

TAS-116

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).

S1175

BIIB021

BIIB021 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.

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.

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.

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.

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.

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.

S8039

PU-H71

PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

S5369

Ethoxyquin

Ethoxyquin is an antioxidant used as a food preservative.

S8365

Apoptozole

Apoptozole is an inhibitor of heat shock protein 70(HSP70) and Hsc70. It induces caspase-dependent apoptosis.

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.

S7750

KNK437

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

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 Kd of 0.48 nM.

S7459

VER-50589

VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.

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. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.

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.

S1972

Tamoxifen Citrate

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding. Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

S1238

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.

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

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.

S5006

Teprenone

Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 2.

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. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.

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.

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.

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.

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.

S7716

TAS-116

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).

S1175

BIIB021

BIIB021 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.

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.

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.

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.

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.

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.

S8039

PU-H71

PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

S5369

Ethoxyquin

Ethoxyquin is an antioxidant used as a food preservative.

S8365

Apoptozole

Apoptozole is an inhibitor of heat shock protein 70(HSP70) and Hsc70. It induces caspase-dependent apoptosis.

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.

S7750

KNK437

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

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 Kd of 0.48 nM.

S7459

VER-50589

VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.

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. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

S1972

Tamoxifen Citrate

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding. Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

2019, 26(3):420-432

2014, Timothy E. Richardson

S1238

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.

2020, 9;11(3):523-535

2020, 130:115123

2020, 9:1503

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1052

Elesclomol (STA-4783)

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

2020, 15;11(1):2423

2020, 54:102715

2020, 12(6):E1645

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.

2020, 185:113230

2019, 10(9):651

2018, 119(1):65-75

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S5006

Teprenone

Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis.

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