EZH1/2

抑制剂选择性比较

EZH1/2产品

所有产品(16) EZH1/2抑制剂(16)

目录号	产品描述	文献引用	实验数据
S7004	EPZ005687 EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。	Nat Commun, 2020, 11(1):604 Gastric Cancer, 2020, 10.1007/s10120-020-01094-0 Theranostics, 2020, 10(19):8494-8512	Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors.
S7164	GSK343 GSK343 是一种有效的，选择性EZH2抑制剂，无细胞试验中IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。GSK343 可诱导自噬。	Nat Commun, 2020, 11(1):3018 Gastric Cancer, 2020, 10.1007/s10120-020-01094-0 Am J Cancer Res, 2020, 1;10(4):1194-1206 eCollection 2020	Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
S7128	Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438)是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。	Oncol Lett, 2021, 21(1):26 Cancer Cell, 2020, 37(2):157-167 Nat Commun, 2020, 11(1):583	EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
S7165	UNC1999 UNC1999 是一种有效的具有口服活性的EZH2和EZH1选择性抑制剂，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。UNC1999 是一种有效的 autophagy 自噬诱导剂。UNC1999 可特异性地抑制H3K27me3/2并诱导一系列抗白血病作用，包括抗增殖、分化和细胞凋亡。	Anticancer Res, 2020, 40(5):2525-2536 Theranostics, 2020, 10(19):8494-8512 Br J Pharmacol, 2019, 10.1111/bph.14754	Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05 (JQEZ5) 是可逆的、特异的EZH1/2抑制剂。	Nat Chem Biol, 2019, 15(4):391-400
S8926^New	Valemetostat (DS-3201) Valemetostat (DS-3201, DS-3201b)是一种选择性的EZH1/2双重抑制剂。
S8353	CPI-1205 CPI-1205是具有口服生物活性的选择性组蛋白赖氨酸甲基转移酶EZH2的抑制剂，对EZH2和EZH1的IC50分别为2 nM和52 nM。它具有潜在的抗肿瘤活性。	Clin Cancer Res, 2019, 10.1158/1078-0432
S9031	Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.	Cancer Lett, 2020, 469:277-286
S7805	EPZ011989 EPZ011989是一种有效的、选择性的、具有口服活性的EZH2抑制剂，Ki值<3 nM。	Cancer Lett, 2020, S0304-3835(20)30632-7 Cancer Cell, 2019, 36(4):385-401 J Cancer, 2018, 9(20):3787-3796
S8702	EBI-2511 EBI-2511是一种有效的、具有口服活性的EZH2抑制剂，对EZH2(A667G)的IC50值为4 nM。
S8494	PF-06726304 PF-06726304是选择性EZH2抑制剂，对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。
S7611	EI1 EI1是一种有效的选择性EZH2抑制剂，对EZH2 (WT)和EZH2 (Y641F)的IC50分别为15 nM和13 nM。	Mol Cancer, 2017, 10.1186/s12943-016-0575-6 Virology, 2017, 506:34-44 Oncotarget, 2015, 6(32):32410-25	EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors.
S7804	GSK503 GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。	Cancer Cell, 2019, 36(4):385-401 J Pathol, 2018, 245(4):433-444 Front Immunol, 2016, 7:496	LC3B‐II levels are increased following 120 h treatment of GSK503 (G, CRMM1 and CRMM2 at 10 μm, and CM2005.1 at 15 μm) or UNC1999 (U, 6 μm).
S7061	GSK126 GSK126 (GSK2816126A, GSK2816126) 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。	Nat Genet, 2020, 52(4):408-417 J Clin Invest, 2020, 3;130(2):853-862 Nat Commun, 2020, 11(1):3018	(C) Four GCBDLBCL cells lines [1 wild-type (wt), 3 mutated (mut) EZH2] were treated with 500 nmol/l BAY 1238097 or with an EZH2 inhibitor (DZNep and GSK126, both used at the concentration of 500 nmol/l) as single agents and in combination for 72 h. The arrow indicates the EZH2 correct band. Dimethyl sulphoxide (DMSO) alone was added as negative control cells. Membranes were hybridized with antibodies against EZH2, H3K27me3, histone H3 and GAPDH.
S7656	CPI-360 CPI-360是一种有效的，选择性的，且SAM竞争性EZH1抑制剂，IC50为102.3 nM，选择性比作用于其它甲基转移酶高100多倍。
S7616	CPI-169 CPI-169是一种有效的选择性EZH2抑制剂，作用于EZH2 WT，EZH2 Y641N，和EZH1的IC50分别为0.24 nM，0.51 nM，和6.1 nM。	J Clin Invest, 2020, 134217 Nat Commun, 2018, 9(1):4116 Virology, 2017, 506:34-44

目录号	产品描述	文献引用	实验数据
S7004	EPZ005687 EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。	Nat Commun,2020, 11(1):604 Gastric Cancer,2020, 10.1007/s10120-020-01094-0 Theranostics,2020, 10(19):8494-8512	Western blot analysis of day 7 lysates from LX92 lysates treated with various EZH2 inhibitors.
S7164	GSK343 GSK343 是一种有效的，选择性EZH2抑制剂，无细胞试验中IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。GSK343 可诱导自噬。	Nat Commun,2020, 11(1):3018 Gastric Cancer,2020, 10.1007/s10120-020-01094-0 Am J Cancer Res,2020, 1;10(4):1194-1206 eCollection 2020	Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
S7128	Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438)是一种有效的，选择性EZH2抑制剂，无细胞试验中K_i 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。	Oncol Lett,2021, 21(1):26 Cancer Cell,2020, 37(2):157-167 Nat Commun,2020, 11(1):583	EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
S7165	UNC1999 UNC1999 是一种有效的具有口服活性的EZH2和EZH1选择性抑制剂，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。UNC1999 是一种有效的 autophagy 自噬诱导剂。UNC1999 可特异性地抑制H3K27me3/2并诱导一系列抗白血病作用，包括抗增殖、分化和细胞凋亡。	Anticancer Res,2020, 40(5):2525-2536 Theranostics,2020, 10(19):8494-8512 Br J Pharmacol,2019, 10.1111/bph.14754	Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05 (JQEZ5) 是可逆的、特异的EZH1/2抑制剂。	Nat Chem Biol,2019, 15(4):391-400
S8926^New	Valemetostat (DS-3201) Valemetostat (DS-3201, DS-3201b)是一种选择性的EZH1/2双重抑制剂。
S8353	CPI-1205 CPI-1205是具有口服生物活性的选择性组蛋白赖氨酸甲基转移酶EZH2的抑制剂，对EZH2和EZH1的IC50分别为2 nM和52 nM。它具有潜在的抗肿瘤活性。	Clin Cancer Res,2019, 10.1158/1078-0432
S9031	Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.	Cancer Lett,2020, 469:277-286
S7805	EPZ011989 EPZ011989是一种有效的、选择性的、具有口服活性的EZH2抑制剂，Ki值<3 nM。	Cancer Lett,2020, S0304-3835(20)30632-7 Cancer Cell,2019, 36(4):385-401 J Cancer,2018, 9(20):3787-3796
S8702	EBI-2511 EBI-2511是一种有效的、具有口服活性的EZH2抑制剂，对EZH2(A667G)的IC50值为4 nM。
S8494	PF-06726304 PF-06726304是选择性EZH2抑制剂，对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。
S7611	EI1 EI1是一种有效的选择性EZH2抑制剂，对EZH2 (WT)和EZH2 (Y641F)的IC50分别为15 nM和13 nM。	Mol Cancer,2017, 10.1186/s12943-016-0575-6 Virology,2017, 506:34-44 Oncotarget,2015, 6(32):32410-25	EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors.
S7804	GSK503 GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。	Cancer Cell,2019, 36(4):385-401 J Pathol,2018, 245(4):433-444 Front Immunol,2016, 7:496	LC3B‐II levels are increased following 120 h treatment of GSK503 (G, CRMM1 and CRMM2 at 10 μm, and CM2005.1 at 15 μm) or UNC1999 (U, 6 μm).
S7061	GSK126 GSK126 (GSK2816126A, GSK2816126) 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。	Nat Genet,2020, 52(4):408-417 J Clin Invest,2020, 3;130(2):853-862 Nat Commun,2020, 11(1):3018	(C) Four GCBDLBCL cells lines [1 wild-type (wt), 3 mutated (mut) EZH2] were treated with 500 nmol/l BAY 1238097 or with an EZH2 inhibitor (DZNep and GSK126, both used at the concentration of 500 nmol/l) as single agents and in combination for 72 h. The arrow indicates the EZH2 correct band. Dimethyl sulphoxide (DMSO) alone was added as negative control cells. Membranes were hybridized with antibodies against EZH2, H3K27me3, histone H3 and GAPDH.
S7656	CPI-360 CPI-360是一种有效的，选择性的，且SAM竞争性EZH1抑制剂，IC50为102.3 nM，选择性比作用于其它甲基转移酶高100多倍。
S7616	CPI-169 CPI-169是一种有效的选择性EZH2抑制剂，作用于EZH2 WT，EZH2 Y641N，和EZH1的IC50分别为0.24 nM，0.51 nM，和6.1 nM。	J Clin Invest,2020, 134217 Nat Commun,2018, 9(1):4116 Virology,2017, 506:34-44

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