HSP (e.g. HSP90)

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

HSP (e.g. HSP90)产品

所有产品 HSP (e.g. HSP90)抑制剂(23) HSP (e.g. HSP90)激活剂(1) HSP (e.g. HSP90)调节剂(3) 新HSP (e.g. HSP90)产品

产品目录	产品描述	文献引用	实验数据
S1141	Tanespimycin (17-AAG) Tanespimycin (17-AAG)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Phase 2。	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 Mol Cell, 2019, 75(4):823-834	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)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Phase 2。	Cancer Cell, 2019, 35(5):752-766 Nat Commun, 2019, 10(1):402 J Neurosci, 2019, 39(17):3332-3344
S1142	Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。	Nat Commun, 2019, 10(1):3562 Mol Cancer Ther, 2019, 18(11):2097-2110 Nat Commun, 2018, 9(1):4296
S1159	Ganetespib (STA-9090) Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 Nat Commun, 2019, 10(1):402	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.
S6721^New	JG98 JG-98是Hsp70的变构抑制剂。
S7716^New	TAS-116 TAS-116是一种新型的HSP90小分子抑制剂，HSP90α和HSP90β的Ki值分别为34.7 nmol/L和21.3 nmol/L。TAS-11并不抑制其他ATP酶，如HSP70(IC50 >200 μmol/L)。
S1175	BIIB021 BIIB021是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，K_i和EC50分别为1.7 nM和38 nM。Phase 2.	SLAS Technol, 2019, 24(1):28-40 Mol Syst Biol, 2018, 14(3):e7858 Endocrinology, 2018, 159(2):907-930
S1163	Onalespib (AT13387) Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。	Nat Commun, 2019, 10(1):5661 Int J Oncol, 2019, 55(6):1287-1295 Prostaglandins Other Lipid Mediat, 2019, 143:106327	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是一种新型的，全部人工合成的HSP90β抑制剂，IC50为58 nM，比作用于Hsp90家族成员Grp94和Trap-1选择性高70倍以上。	Nat Commun, 2017, 8(1):422 Mol Cancer, 2017, 16(1):72 Cell Death Dis, 2016, 7:e2051	Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).
S2713	Geldanamycin Geldanamycin是一种天然的HSP90抑制剂，K_d为1.2 μM，特异性干扰糖皮质激素受体（GR）/HSP联合。	Nat Commun, 2019, 10(1):2131 Autophagy, 2019, 15(9):1558-1571 Autophagy, 2019, 15(9):1558-1571	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)选择性结合到HSP90α和HSP90β的ATP结合袋中，K_a分别为30 nM和30 nM，比17-AAG更有效。	Nat Commun, 2019, 10(1):402 Int J Biol Sci, 2019, 15(2):312-324 Anticancer Res, 2018, 38(9):5177-5181
S2656	PF-04929113 (SNX-5422) PF-04929113 (SNX-5422)是一种有效的，选择性的HSP90抑制剂，K_d为41 nM，且诱导Her-2降解，IC50为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是一种非Ansamycin的HSP90抑制剂，IC50为3.8 nM。Phase 1。	Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
S7122	XL888 XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。Phase 1	Oncotarget, 2016, 7(31):49597-49610 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 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。	Theranostics, 2019, 9(2):554-572 Onco Targets Ther, 2018, 11:1583-1593 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是有效的选择性HSP90抑制剂，IC50为51 nM。	PLoS Pathog, 2018, 14(5):e1007058 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是热激蛋白HSP70和Hsc70的抑制剂，与HSP70和Hsc70的Kd值分别为0.14 μM和0.21 μM。它能够诱导caspase依赖性的凋亡反应。	Nat Commun, 2018, 9(1):4700 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抑制热激诱导的荧光素酶活性，IC50为1.2 μM。它是转录因子热休克因子1(HSF1)的抑制剂。	Theranostics, 2019, 9(10):2999-3013
S7750	KNK437 KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。	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 是一种强效的HSP90抑制剂，其IC50为 47 nM。
S7340	CH5138303 CH5138303 是口服有效的Hsp90抑制剂，其K_d为 0.48 nM。
S7459	VER-50589 VER-50589 是强效的HSP90抑制剂，对HSP90β的IC50为21 nM。	PLoS Negl Trop Dis, 2014, 8(2):e2699
S7751	VER155008 VER-155008是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。	Biochim Biophys Acta Mol Cell Res, 2019, 1866(10):1544-1555 Nat Commun, 2018, 9(1):4700 Cancer Sci, 2018, 109(2):373-383	(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).
S6568^New	ML346 ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。
S1052	Elesclomol (STA-4783) Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。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是heat shock protein 70 (HSP70)的诱导物，同时也是有效的抗炎药。
S8299	HA15 HA15是特异靶向BiP/GRP78/HSPA5的小分子。在所检测的黑色素瘤细胞中具有抗肿瘤活性，包括从病人中分离得到的细胞和对BRAF抑制剂具有耐药性的细胞。	Cell Death Dis, 2019, 10(9):651 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.

产品目录	产品描述	文献引用	实验数据
S1141	Tanespimycin (17-AAG) Tanespimycin (17-AAG)是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Phase 2。	Cell,2019, 36(2):179-193 Cancer Cell,2019, 36(2):179-193 Mol Cell,2019, 75(4):823-834	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)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Phase 2。	Cancer Cell,2019, 35(5):752-766 Nat Commun,2019, 10(1):402 J Neurosci,2019, 39(17):3332-3344
S1142	Alvespimycin (17-DMAG) HCl Alvespimycin (17-DMAG) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。	Nat Commun,2019, 10(1):3562 Mol Cancer Ther,2019, 18(11):2097-2110 Nat Commun,2018, 9(1):4296
S1159	Ganetespib (STA-9090) Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。	Cell,2019, 36(2):179-193 Cancer Cell,2019, 36(2):179-193 Nat Commun,2019, 10(1):402	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.
S6721^New	JG98 JG-98是Hsp70的变构抑制剂。
S7716^New	TAS-116 TAS-116是一种新型的HSP90小分子抑制剂，HSP90α和HSP90β的Ki值分别为34.7 nmol/L和21.3 nmol/L。TAS-11并不抑制其他ATP酶，如HSP70(IC50 >200 μmol/L)。
S1175	BIIB021 BIIB021是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，K_i和EC50分别为1.7 nM和38 nM。Phase 2.	SLAS Technol,2019, 24(1):28-40 Mol Syst Biol,2018, 14(3):e7858 Endocrinology,2018, 159(2):907-930
S1163	Onalespib (AT13387) Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。	Nat Commun,2019, 10(1):5661 Int J Oncol,2019, 55(6):1287-1295 Prostaglandins Other Lipid Mediat,2019, 143:106327	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是一种新型的，全部人工合成的HSP90β抑制剂，IC50为58 nM，比作用于Hsp90家族成员Grp94和Trap-1选择性高70倍以上。	Nat Commun,2017, 8(1):422 Mol Cancer,2017, 16(1):72 Cell Death Dis,2016, 7:e2051	Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).
S2713	Geldanamycin Geldanamycin是一种天然的HSP90抑制剂，K_d为1.2 μM，特异性干扰糖皮质激素受体（GR）/HSP联合。	Nat Commun,2019, 10(1):2131 Autophagy,2019, 15(9):1558-1571 Autophagy,2019, 15(9):1558-1571	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)选择性结合到HSP90α和HSP90β的ATP结合袋中，K_a分别为30 nM和30 nM，比17-AAG更有效。	Nat Commun,2019, 10(1):402 Int J Biol Sci,2019, 15(2):312-324 Anticancer Res,2018, 38(9):5177-5181
S2656	PF-04929113 (SNX-5422) PF-04929113 (SNX-5422)是一种有效的，选择性的HSP90抑制剂，K_d为41 nM，且诱导Her-2降解，IC50为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是一种非Ansamycin的HSP90抑制剂，IC50为3.8 nM。Phase 1。	Clin Exp Med,2019, 10.1007/s10238-019-00587-2
S7122	XL888 XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。Phase 1	Oncotarget,2016, 7(31):49597-49610 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 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。	Theranostics,2019, 9(2):554-572 Onco Targets Ther,2018, 11:1583-1593 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是有效的选择性HSP90抑制剂，IC50为51 nM。	PLoS Pathog,2018, 14(5):e1007058 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是热激蛋白HSP70和Hsc70的抑制剂，与HSP70和Hsc70的Kd值分别为0.14 μM和0.21 μM。它能够诱导caspase依赖性的凋亡反应。	Nat Commun,2018, 9(1):4700 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抑制热激诱导的荧光素酶活性，IC50为1.2 μM。它是转录因子热休克因子1(HSF1)的抑制剂。	Theranostics,2019, 9(10):2999-3013
S7750	KNK437 KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。	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 是一种强效的HSP90抑制剂，其IC50为 47 nM。
S7340	CH5138303 CH5138303 是口服有效的Hsp90抑制剂，其K_d为 0.48 nM。
S7459	VER-50589 VER-50589 是强效的HSP90抑制剂，对HSP90β的IC50为21 nM。	PLoS Negl Trop Dis,2014, 8(2):e2699
S7751	VER155008 VER-155008是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。	Biochim Biophys Acta Mol Cell Res,2019, 1866(10):1544-1555 Nat Commun,2018, 9(1):4700 Cancer Sci,2018, 109(2):373-383	(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).

产品目录	产品描述	文献引用	实验数据
S6568^New	ML346 ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。

产品目录

产品描述

文献引用

实验数据

S6568^New

ML346

ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。

产品目录	产品描述	文献引用	实验数据
S1052	Elesclomol (STA-4783) Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。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是heat shock protein 70 (HSP70)的诱导物，同时也是有效的抗炎药。
S8299	HA15 HA15是特异靶向BiP/GRP78/HSPA5的小分子。在所检测的黑色素瘤细胞中具有抗肿瘤活性，包括从病人中分离得到的细胞和对BRAF抑制剂具有耐药性的细胞。	Cell Death Dis, 2019, 10(9):651 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.

产品目录

产品描述

文献引用

实验数据

S1052