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(21) HSP (e.g. HSP90)调节剂(3)

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。	Mol Cell, 2013, 50(3):368-78 J Exp Med, 2012, 209(2):259-73 P Natl Acad Sci USA, 2011, 108(18):7535-40	(A) Cell lines were seeded in 96-well plates and treated with 10 nM of 17-AAG for 72 h. Cell survival was analyzed using CellTiter-Glo. Both parental H3122 cells (red bar) and H3122 CR cells (blue bar) show sensitivity to 17-AAG. (B) Suppression of ALK signaling by 17-AAG in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of 17-AAG for 6 h.
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。	Nat Med, 2015, 10.1038/nm.3855 Nat Commun, 2014, 5:3361 Proc Natl Acad Sci USA, 2014, 111(15):E1528-37	U2OS_exo cells were incubated with AUY922 for 20 h at the indicated concentrations before stimulation with TNFα (30 ng/mL) for 30 min and immunostaining to detect NF-κB (p65). DMSO 1%, cells stimulated by TNFα in the absence of AUY922. Representative pictures used to quantify nuclear and cytoplasmic localization of NF-κB.
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。	Hepatology, 2013, 57(1):70-80 J Thorac Oncol, 2012, 7(7):1078-85 Cell Death Dis, 2016, 7(6):e2290	H2228/Vec or H2228/HGF cells were treated with or without alectinib (0.3 μmol/L) for 2 h or 17-DMAG (0.3 μmol/L) for 24 h and then stimulated with or without HGF (50 ng/mL) for 10 minutes. The resultant cells were lysed, and the indicated proteins were detected by immunoblotting.
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。	Nature, 2017, 10.1038/nature21064 Cell, 2017, 168(5):856-866 Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1017	Loss of viability (Z score) resulting from HSP90 inhibition (HSP90i; ganetespib, 5 nM) in FANCA null GM6914 cells transduced with retroviruses encoding FANCA wild-type (squares; WT) or empty vector control (circles; null) in the presence (black symbols) of MMC (31.6 nM) or DMSO control (gray symbols). Data from three independent experiments are presented as mean ± SEM.
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.	Cell, 2017, 168(5):856-866 Arthritis Rheumatol , 2013, 65(8):2102-12 PLoS Pathog, 2012, 8(11):e1003048
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。	Cell, 2017, 168(5):856-866 PLoS One, 2013, 8(4):e59315 PLoS One, 2017, 12(5):e0177878	Relative effect of pharmacological HSP90 inhibition by (B) onalespib (AT13387, 10-40 nM) on the viability of FANCA wild-type and FANCA null cells under normal conditions or with increasing concentrations of MMC. Left panels indicate the effects of the indicated inhibitor on cell growth; middle panels the effects onMMCtolerance in FANCA-wild-type cells; right panels the effects onMMCtolerance in FANCA null cells Data presented as the mean ± SEM from 2 independent experiments.
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。	Cancer Cell, 2012, 20(3):400-13 Mol Cancer, 2017, 16(1):72 PLoS Pathog, 2012, 8(11):e1003048	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。	J Antimicrob Chemother, 2015, 10.1093/jac/dku549 Antimicrob Agents Chemother, 2015, 59(8):4727-33 PLoS One, 2015, 10(9):e0138936	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。	PLoS Negl Trop Dis, 2014, 8(2):e2699 Mol Cell Biol, 2013, 33(12):2375-87 Immunopharmacol Immunotoxicol, 2015, 8:1-10
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。	Antimicrob Agents Chemother, 2014, 58(7):4138-44 J Biol Chem, 2013, 288(23):16308-20 Endocrine, 2016, 51(2):274-82	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。
S7122	XL888 XL888一种ATP竞争性的HSP90抑制剂，IC50为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 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 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。	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。	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。
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。	Cell Signal, 2017, 30:130-141 Neuroscience, 2014, 281C:164-177 Br J Haematol, 2016, 175(4):641-651	RD cells were pre-treated with Ver-155008 for 2 hours at indicated concentration following an infection of EV-A71 at MOI of 10 for 9 hours. Proteins levels of VP0/2 by western blot.
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。	Cell, 2017, 168(1-2):86-100 Osteoporos Int, 2018, 29(8):1917-1926 BMC Genomics, 2014, 15(1):263	Treatment with elesclomol inhibits cancer cell growth and induces apoptosis by increasing ROS levels. a. Cell growth of SMOV2, IGROV1, and OVCA432 ovarian cancer cells treated with elesclomol in the presence or absence of the antioxidant NAC for 72 h. Cell growth was measured using the WST-1 assay and quantified relative to DMSO treated controls.
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。	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。	Mol Cell,2013, 50(3):368-78 J Exp Med,2012, 209(2):259-73 P Natl Acad Sci USA,2011, 108(18):7535-40	(A) Cell lines were seeded in 96-well plates and treated with 10 nM of 17-AAG for 72 h. Cell survival was analyzed using CellTiter-Glo. Both parental H3122 cells (red bar) and H3122 CR cells (blue bar) show sensitivity to 17-AAG. (B) Suppression of ALK signaling by 17-AAG in resistant H3122 CR cells. H3122 parental and resistant cells were exposed to increasing concentrations of 17-AAG for 6 h.
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。	Nat Med,2015, 10.1038/nm.3855 Nat Commun,2014, 5:3361 Proc Natl Acad Sci USA,2014, 111(15):E1528-37	U2OS_exo cells were incubated with AUY922 for 20 h at the indicated concentrations before stimulation with TNFα (30 ng/mL) for 30 min and immunostaining to detect NF-κB (p65). DMSO 1%, cells stimulated by TNFα in the absence of AUY922. Representative pictures used to quantify nuclear and cytoplasmic localization of NF-κB.
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。	Hepatology,2013, 57(1):70-80 J Thorac Oncol,2012, 7(7):1078-85 Cell Death Dis,2016, 7(6):e2290	H2228/Vec or H2228/HGF cells were treated with or without alectinib (0.3 μmol/L) for 2 h or 17-DMAG (0.3 μmol/L) for 24 h and then stimulated with or without HGF (50 ng/mL) for 10 minutes. The resultant cells were lysed, and the indicated proteins were detected by immunoblotting.
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。	Nature,2017, 10.1038/nature21064 Cell,2017, 168(5):856-866 Cancer Res,2014, 10.1158/0008-5472.CAN-14-1017	Loss of viability (Z score) resulting from HSP90 inhibition (HSP90i; ganetespib, 5 nM) in FANCA null GM6914 cells transduced with retroviruses encoding FANCA wild-type (squares; WT) or empty vector control (circles; null) in the presence (black symbols) of MMC (31.6 nM) or DMSO control (gray symbols). Data from three independent experiments are presented as mean ± SEM.
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.	Cell,2017, 168(5):856-866 Arthritis Rheumatol ,2013, 65(8):2102-12 PLoS Pathog,2012, 8(11):e1003048
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。	Cell,2017, 168(5):856-866 PLoS One,2013, 8(4):e59315 PLoS One,2017, 12(5):e0177878	Relative effect of pharmacological HSP90 inhibition by (B) onalespib (AT13387, 10-40 nM) on the viability of FANCA wild-type and FANCA null cells under normal conditions or with increasing concentrations of MMC. Left panels indicate the effects of the indicated inhibitor on cell growth; middle panels the effects onMMCtolerance in FANCA-wild-type cells; right panels the effects onMMCtolerance in FANCA null cells Data presented as the mean ± SEM from 2 independent experiments.
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。	Cancer Cell,2012, 20(3):400-13 Mol Cancer,2017, 16(1):72 PLoS Pathog,2012, 8(11):e1003048	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。	J Antimicrob Chemother,2015, 10.1093/jac/dku549 Antimicrob Agents Chemother,2015, 59(8):4727-33 PLoS One,2015, 10(9):e0138936	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。	PLoS Negl Trop Dis,2014, 8(2):e2699 Mol Cell Biol,2013, 33(12):2375-87 Immunopharmacol Immunotoxicol,2015, 8:1-10
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。	Antimicrob Agents Chemother,2014, 58(7):4138-44 J Biol Chem,2013, 288(23):16308-20 Endocrine,2016, 51(2):274-82	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。
S7122	XL888 XL888一种ATP竞争性的HSP90抑制剂，IC50为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 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 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。	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。	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。
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。	Cell Signal,2017, 30:130-141 Neuroscience,2014, 281C:164-177 Br J Haematol,2016, 175(4):641-651	RD cells were pre-treated with Ver-155008 for 2 hours at indicated concentration following an infection of EV-A71 at MOI of 10 for 9 hours. Proteins levels of VP0/2 by western blot.

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。	Cell, 2017, 168(1-2):86-100 Osteoporos Int, 2018, 29(8):1917-1926 BMC Genomics, 2014, 15(1):263	Treatment with elesclomol inhibits cancer cell growth and induces apoptosis by increasing ROS levels. a. Cell growth of SMOV2, IGROV1, and OVCA432 ovarian cancer cells treated with elesclomol in the presence or absence of the antioxidant NAC for 72 h. Cell growth was measured using the WST-1 assay and quantified relative to DMSO treated controls.
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。	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