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Search Results for " ezh2 inhibitor "

59

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T2079	GSK126 GSK2816126A,EZH2 inhibitor	Histone Methyltransferase	Chromatin/Epigenetic
	GSK126 (GSK2816126A) 是一种选择性的EZH2甲基转移酶抑制剂，IC50为 9.9 nM。
T6484	EI1 KB-145943,Ezh2 inhibitor	Apoptosis; Histone Methyltransferase	Apoptosis; Chromatin/Epigenetic
	EI1 (Ezh2 inhibitor) 是一种EZH2抑制剂，能够作用于 EZH2 (WT) 和 EZH2 (Y641F)，IC50值分别为 15 nM 和 13 nM。
T7305	JQEZ5	Histone Methyltransferase	Chromatin/Epigenetic
	JQEZ5 是一种选择性EZH2赖氨酸甲基转移酶抑制剂，具有抗肿瘤作用。它以 SAM 竞争性方式抑制PRC2的酶功能，IC50为 80 nM。
T12428L	PF-06726304	Histone Methyltransferase	Chromatin/Epigenetic
	PF-06726304 是选择性EZH2有效抑制剂，具有强抗肿瘤生长活性。它抑制野生型和 Y641N 突变型 EZH2，Ki 分别为 0.7 和 3.0 nM。
T25400	EZH2-IN-3 EZH2 inhibitor 3,EZH2-inhibitor-3
	EZH2-IN-3 is an inhibitor of EZH2 and EZH1 with selective impact on diffuse large B cell lymphoma cell growth.
T1788	Tazemetostat E-7438,EPZ6438	Histone Methyltransferase	Chromatin/Epigenetic
	Tazemetostat (EPZ6438) 是一种组蛋白甲基转移酶 EZH2 抑制剂 (IC50=11 nM)，具有口服活性、选择性和 SAM 竞争性。Tazemetostat 具有抗肿瘤活性，可以用于治疗上皮样肉瘤/滤泡性淋巴瘤。
T17002	Tazemetostat hydrobromide E-7438 hydrobromide,氢溴酸泰泽司他,EPZ-6438 hydrobromide	Histone Methyltransferase	Chromatin/Epigenetic
	Tazemetostat hydrobromide (E-7438 hydrobromide) 是口服的EZH2选择性抑制剂。它抑制含有 PRC2 复合体的野生型 EZH2 的活性，Ki 为 2.5 nM。它还抑制 EZH1，IC50为 392 nM。
T64043	EZH2-IN-13	Histone Methyltransferase	Chromatin/Epigenetic
	EZH2-IN-13 是一种有效的 EZH2 抑制剂，具有潜在的抗癌活性。EZH2-IN-13 可用于研究与 EZH2 活性相关的疾病。
T6809	CPI-169 racemate CPI 169,CPI-169,CPI169	Epigenetic Reader Domain; Histone Methyltransferase	Chromatin/Epigenetic
	CPI-169 racemate (CPI 169) 是CPI-169的消旋体。CPI-169 是一种有效的选择性 EZH2 抑制剂，对 EZH2 WT、EZH2 Y641N 和 EZH1 的 IC50 分别为 0.24、0.51 和 6.1 nM。
T67883	EZH2-IN-15 SHR2554	Histone Methyltransferase	Chromatin/Epigenetic
	EZH2-IN-15 是zeste 2组蛋白修饰增强子(EZH2)的特异性抑制剂。EZH2在许多人类癌症中异常过表达，通过调节Treg 活性来控制适应性反应。肿瘤内EZH2的表达也被证明可以控制先天免疫
T2435	EPZ011989	Histone Methyltransferase	Chromatin/Epigenetic
	EPZ011989是一种高选择性可口服的 EZH2抑制剂，对wt EZH2以及EZH2突变型Ki 值<3nM。
T9700	EZH2-IN-2	Histone Methyltransferase	Chromatin/Epigenetic
	EZH2-IN-2 是一种 EZH2 抑制剂，IC50 值为 64 nM。EZH2-IN-2 可用于研究与 EZH2 活性相关的癌症或癌前病变。
T6360	3-deazaneplanocin A HCl	Others; Histone Methyltransferase	Chromatin/Epigenetic; Others
	3-deazaneplanocin A HCl 是组蛋白甲基转移酶 (EZH2) 和 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。
T15194	EBI-2511	Histone Methyltransferase	Chromatin/Epigenetic
	EBI-2511 是一种高效且具有口服活性的 EZH2 抑制剂，在 Pfeffiera 细胞系中的 IC50值为 6 nM。
T1775	GSK503	Histone Methyltransferase	Chromatin/Epigenetic
	GSK503是一种高效特异性EZH2甲基转移酶抑制剂，Ki 值为3到27 nM，具有潜在的抗肿瘤活性。
T60194	N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide	Histone Methyltransferase	Chromatin/Epigenetic
	N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide 是一种强效的、选择性的Enhancer of Zeste Homolog 2 (EZH2)，对EZH2 WT 和EZH2-Y641F 的IC50分别为37.6nM 和79.1nM。
T1905	EPZ005687	Histone Methyltransferase	Chromatin/Epigenetic
	EPZ005687 是一种选择性EZH2抑制剂，Ki 值为 24 nM，对其选择性是对 EZH1 的 50 倍，对其他 15 种甲基转移酶的 500 倍。
T12430	PF-06821497	Histone Methyltransferase	Chromatin/Epigenetic
	PF-06821497 是一种特异性的 EZH2 抑制剂，具有显着的肿瘤生长抑制作用。
T3057	UNC1999	Histone Methyltransferase; Autophagy	Autophagy; Chromatin/Epigenetic
	UNC1999 是一种可口服的，选择性和 SAM-竞争性的 EZH2和 EZH1抑制剂，IC50分别为 <10 nM 和 45 nM。
T8510	CPI-1205 Lirametostat	Histone Methyltransferase	Chromatin/Epigenetic
	CPI-1205 是一种高效的选择性 EZH2 抑制剂（IC50：0.002 μM，EC50：0.032 μM）。
T6810	CPI-360 Synonym 2,CPI 360,CPI360	Apoptosis; Histone Methyltransferase	Apoptosis; Chromatin/Epigenetic
	CPI-360是一种小分子EZH2抑制剂（IC50：0.002 μM，EC50： 0.080μM），在EZH200依赖性肿瘤异种移植模型中显示出抗肿瘤活性。
T6059	GSK343	Histone Methyltransferase; Autophagy	Autophagy; Chromatin/Epigenetic
	GSK343 是一种特异性且有效的 EZH2 抑制剂，IC50为 4 nM。它对 EZH1 的特异性活性是 60 倍。
T29231	ZLD1039 ZLD-1039,ZLD 1039	Histone Methyltransferase	Chromatin/Epigenetic
	ZLD1039 是一种口服有效的、高选择性 EZH2 抑制剂。ZLD1039 高效抑制 EZH2 野生型及 Y641F 和 A677G 突变型，IC50 分别为 5.6、15 和 4.0 nM。ZLD1039 抑制乳腺肿瘤的生长和转移。
T25471	GSK-A GSK A
	GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor.
T12428	PF-06726304 acetate	Histone Methyltransferase	Chromatin/Epigenetic
	PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
T38827	EZH2-IN-5 EZH2-IN-5
	EZH2-IN-5 is a highly effective inhibitor of EZH2, displaying remarkable potency against both wild-type and mutant Tyr641 EZH2, with IC50 values of 1.52 nM and 4.07 nM, respectively.
T40323	EZH2-IN-6 EZH2-IN-6
	EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity.
T39497	EZH2-IN-4 EZH2-IN-4
	EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.
T39971	CPI-1328
	CPI-1328 is an EZH2 inhibitor with a K i value of 63 fM.
T64307	EZH2-IN-8
	EZH2-IN-8 是一种 EZH2 的有效抑制剂。其中 EZH2 过表达或 SET 区突变 (Y641F、Y641N、A687V、A677G 点突变) 都会造成 H3K27me3 异常升高，诱导多种肿瘤（如乳腺癌、前列腺癌、白血病等）的生长发育。EZH2-IN-8 具有潜力进行癌症疾病的研究。
T40310	PARP/EZH2-IN-1 PARP/EZH2-IN-1
	PARP/EZH2-IN-1 is a novel compound that functions as a dual inhibitor for both PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for the treatment of triple-negative breast cancer with wild-type BRCA.
T27069	CPI-169 CPI 169 (R),CPI-169 (R)
	CPI-169 (R) is a novel and potent inhibitor of EZH2.
T25470	GSK926 GSK 926,GSK-926
	GSK926 is a selective, SAM-competitive, and cell-active EZH2 inhibitor.
T62896	EZH2-IN-12
	EZH2-IN-12 (Compound 5) 是一种 EZH2 的有效抑制剂。EZH2-IN-12 具有潜力进行中枢神经系统恶性肿瘤的研究。
T29232	ZLD10A ZLD 10 A,ZLD-10-A
	ZLD10A is a highly potent and selective small molecule inhibitor of EZH2.
T27074	CPI-905 CPI 905
	CPI-905 is a potent and selective EZH2 inhibitor with IC50 value of 39.5 nM.
T69771	MS-177
	MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
T73246	EZH2-IN-7
	EZH2-IN-7 是一种有效的EZH2抑制剂。EZH2过表达或 SET 区突变 (Y641F、Y641N、A687V、A677G 点突变) 均导致H3K27me3异常升高，促进多种肿瘤的生长发育，如乳腺癌、前列腺癌、白血病等。EZH2-IN-7 具有研究癌症疾病的潜力。
T27130	DCE_42 DCE 42,DCE42,DCE-42
	DCE_42 is a novel EZH2 inhibitor, it also displays significant anti-proliferation activity against lymphoma cell lines.
T11436	GNA002	Histone Methyltransferase	Chromatin/Epigenetic
	GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
T15240	Tazemetostat trihydrochloride EPZ-6438 trihydrochloride,E-7438 trihydrochloride	Histone Methyltransferase	Chromatin/Epigenetic
	Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo
T74602	PROTAC EZH2 Degrader-1
	PROTACEZH2 Degrader-1 (Compound 150d)是高效的PROTACEZH2降解剂，能够抑制EZH2甲基转移酶的活性，其IC50值为2.7 nM。由于EZH2在许多肿瘤的发生及进展中具有关键作用，这种化合物的研发具有重要意义。
T69264	Aristeromycin diphosphate
	Aristeromycin diphosphate is an inhibitor of S-adenosylhomocysteine hydrolase (AHCY), inducing miR-26a and regulating oncogenic EZH2 expression, showing high inhibitory activity against AHCY, and causing growth inhibition of prostate cancer.
T73116	(R)-HH2853
	(R)-HH2853 是一种突变型EZH2抑制剂，对EZH2-Y641F 的IC50<100 nM。(R)-HH2853 可用于癌症和自身免疫性疾病。
T79849	Igermetostat	Histone Methyltransferase	Chromatin/Epigenetic
	Igermetostat为EZH2抑制剂，适用于体内外癌症研究。
T2435L	EPZ011989 HCl(1598383-40-4 Free base) EPZ-011989 TFA,EPZ011989 TFA salt,EPZ 011989 TFA,EPZ011989 TFA
	EPZ011989为一高效选择性口服EZH2抑制剂，Ki值<3 nM。
T27129	DCE_254 DCE 254,DCE-254,DCE254
	DCE_254 is a novel EZH2 inhibitor, it also displays significant anti-proliferation activity against lymphoma cell lines.
T70588	Tazemetostat HCl
	Tazemetostat HCl is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation. These data demonstrate the dependency of SMARCB1...
T73134	EZH2-IN-14
	EZH2-IN-14为一种选择性EZH2(Histone Methyltransferase)抑制剂，具IC50值12 nM。该化合物通过抑制EZH2/PRC2的甲基转移酶活性（减少H3K27me3），显著抑制其功能。相比高度同源的H3K27甲基转移酶EZH1，EZH2-IN-14对EZH2的选择性提高200倍以上。
T63970	EZH2-IN-11
	EZH2-IN-11 是 E2HZ 的有效抑制剂。其中 EZH2 的致癌活性已被各种不同癌症类型中的大量研究中证实。EZH2-IN-11 对癌症疾病表现出研究潜力。

化合物

Cat.No: T2079

Synonym: GSK2816126A,EZH2 inhibitor

Target: Histone Methyltransferase

Cat.No: T6484

Synonym: KB-145943,Ezh2 inhibitor

Target: Apoptosis, Histone Methyltransferase

Cat.No: T7305

Target: Histone Methyltransferase

Cat.No: T12428L

Target: Histone Methyltransferase

Cat.No: T25400

Synonym: EZH2 inhibitor 3,EZH2-inhibitor-3

Cat.No: T1788

Synonym: E-7438,EPZ6438

Target: Histone Methyltransferase

Tazemetostat hydrobromide

Cat.No: T17002

Synonym: E-7438 hydrobromide,氢溴酸泰泽司他,EPZ-6438 hydrobromide

Target: Histone Methyltransferase

Cat.No: T64043

Target: Histone Methyltransferase

CPI-169 racemate

Cat.No: T6809

Synonym: CPI 169,CPI-169,CPI169

Target: Epigenetic Reader Domain, Histone Methyltransferase

Cat.No: T67883

Synonym: SHR2554

Target: Histone Methyltransferase

Cat.No: T2435

Target: Histone Methyltransferase

Cat.No: T9700

Target: Histone Methyltransferase

3-deazaneplanocin A HCl

Cat.No: T6360

Target: Others, Histone Methyltransferase

Cat.No: T15194

Target: Histone Methyltransferase

Cat.No: T1775

Target: Histone Methyltransferase

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide

Cat.No: T60194

Target: Histone Methyltransferase

Cat.No: T1905

Target: Histone Methyltransferase

Cat.No: T12430

Target: Histone Methyltransferase

Cat.No: T3057

Target: Histone Methyltransferase, Autophagy

Cat.No: T8510

Synonym: Lirametostat

Target: Histone Methyltransferase

Cat.No: T6810

Synonym: Synonym 2,CPI 360,CPI360

Target: Apoptosis, Histone Methyltransferase

Cat.No: T6059

Target: Histone Methyltransferase, Autophagy

Cat.No: T29231

Synonym: ZLD-1039,ZLD 1039

Target: Histone Methyltransferase

Cat.No: T25471

Synonym: GSK A

PF-06726304 acetate

Cat.No: T12428

Target: Histone Methyltransferase

Cat.No: T38827

Synonym: EZH2-IN-5

Cat.No: T40323

Synonym: EZH2-IN-6

Cat.No: T39497

Synonym: EZH2-IN-4

Cat.No: T39971

Cat.No: T64307

PARP/EZH2-IN-1

Cat.No: T40310

Synonym: PARP/EZH2-IN-1

Cat.No: T27069

Synonym: CPI 169 (R),CPI-169 (R)

Cat.No: T25470

Synonym: GSK 926,GSK-926

Cat.No: T62896

Cat.No: T29232

Synonym: ZLD 10 A,ZLD-10-A

Cat.No: T27074

Synonym: CPI 905

Cat.No: T69771

Cat.No: T73246

Cat.No: T27130

Synonym: DCE 42,DCE42,DCE-42

Cat.No: T11436

Target: Histone Methyltransferase

Tazemetostat trihydrochloride

Cat.No: T15240

Synonym: EPZ-6438 trihydrochloride,E-7438 trihydrochloride

Target: Histone Methyltransferase

PROTAC EZH2 Degrader-1

Cat.No: T74602

Aristeromycin diphosphate

Cat.No: T69264

Cat.No: T73116

Cat.No: T79849

Target: Histone Methyltransferase

EPZ011989 HCl(1598383-40-4 Free base)

Cat.No: T2435L

Synonym: EPZ-011989 TFA,EPZ011989 TFA salt,EPZ 011989 TFA,EPZ011989 TFA

Cat.No: T27129

Synonym: DCE 254,DCE-254,DCE254

Tazemetostat HCl

Cat.No: T70588

Cat.No: T73134

Cat.No: T63970

Cat. No.	Product Name	Target	Signaling Pathways
T8201	Gambogenic acid	Histone Methyltransferase	Chromatin/Epigenetic
	Gambogenic acid 是黄藤中的一种有效成分，具有抗癌活性。它是特异性EZH2抑制剂，与 EZH2-SET 结构域的 Cys668 位点共价结合，诱导 EZH2 泛素化。

天然产物

Gambogenic acid

Cat.No: T8201

Target: Histone Methyltransferase

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