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72

抑制剂 & 化合物

3

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。
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。
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.
T40323	EZH2-IN-6 EZH2-IN-6
	EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor 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.
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.
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.
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
TP2115	SAH-EZH2
	EZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
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。
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。
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。
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。
T79780	IHMT-EZH2-426	Histone Methyltransferase	Chromatin/Epigenetic
	IHMT-EZH2-426（compound 38）是一种针对EZH2野生型及其A687V和Y641F/Y641N/Y641S突变体高效的共价降解剂，其IC50值分别为1.3 nM、1.2 nM以及1.7-3.5 nM。该化合物通过下调H3K27me3和EZH2蛋白表达水平，显著抑制B细胞淋巴瘤和三阴性乳腺癌（TNBC）细胞系的增殖。
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。
T64208	EZH2-IN-9
	EZH2-IN-9 是一种 EZH2 的有效抑制剂。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，促使多种肿瘤（如乳腺癌、前列腺癌、白血病等）的生长发育。EZH2-IN-9 对癌症疾病表现出研究潜力。
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。
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。
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。
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。
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。
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。
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。
T13780	MS1943	Apoptosis; Histone Methyltransferase	Apoptosis; Chromatin/Epigenetic
	MS1943 是一种具有口服生物活性的 EZH2选择性降解剂，IC50为 120 nM。它显著降低了许多三阴性乳腺癌和其他癌及非癌细胞系中的 EZH2蛋白水平，能有效阻止多个三阴性乳腺癌和其他癌细胞系的增殖。
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。
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）。
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。
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。
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。
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。
T40199	Tulmimetostat CPI-0209	Histone Methyltransferase	Chromatin/Epigenetic
	Tulmimetostat (CPI-0209) 是一种具有口服活性的 EZH1/EZH2 抑制剂。Tulmimetostat 有抗肿瘤活性，用于研究卵巢癌和晚期实体瘤。
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。
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。
T10205	A-395	Histone Methyltransferase	Chromatin/Epigenetic
	A-395 是一种多梳抑制复合物 2 (PRC2) 蛋白质-蛋白质相互作用的拮抗剂，可有效抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12)，IC50为 18 nM。
T12428	PF-06726304 acetate	Histone Methyltransferase	Chromatin/Epigenetic
	PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
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
T40038	UNC2399 UNC2399
	UNC2399, a biotinylated version of UNC1999, functions as a selective degrader of EZH2 and exhibits strong in vitro efficacy against EZH2, demonstrated by its IC 50 value of 17 nM.
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).
T27069	CPI-169 CPI 169 (R),CPI-169 (R)
	CPI-169 (R) is a novel and potent inhibitor of EZH2.
T79200	BBDDL2059	Histone Methyltransferase	Chromatin/Epigenetic
	BBDDL2059为一选择性组蛋白甲基转移酶EZH2共价抑制剂，具EZH2-Y641F IC50值1.5 nM。该化合物能于纳摩尔浓度抑制淋巴瘤细胞生长，适应于抗癌研究。
T25471	GSK-A GSK A
	GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor.
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。
T39971	CPI-1328
	CPI-1328 is an EZH2 inhibitor with a K i value of 63 fM.
T36799	UNC 2399
	Biotinylated UNC 1999 (Cat.No. 4904, IC50 = 17 nM). Enriches lysine methyltransferase EZH2 from HEK293T cells. Negative control also avilable. 0
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.

化合物

Cat.No: T9700

Target: Histone Methyltransferase

Cat.No: T6484

Synonym: KB-145943,Ezh2 inhibitor

Target: Apoptosis, Histone Methyltransferase

Cat.No: T2079

Synonym: GSK2816126A,EZH2 inhibitor

Target: Histone Methyltransferase

Cat.No: T64043

Target: Histone Methyltransferase

Cat.No: T25400

Synonym: EZH2 inhibitor 3,EZH2-inhibitor-3

Cat.No: T40323

Synonym: EZH2-IN-6

Cat.No: T38827

Synonym: EZH2-IN-5

Cat.No: T39497

Synonym: EZH2-IN-4

PARP/EZH2-IN-1

Cat.No: T40310

Synonym: PARP/EZH2-IN-1

Cat.No: T67883

Synonym: SHR2554

Target: Histone Methyltransferase

Cat.No: TP2115

PROTAC EZH2 Degrader-1

Cat.No: T74602

Cat.No: T73246

Cat.No: T62896

Cat.No: T64307

IHMT-EZH2-426

Cat.No: T79780

Target: Histone Methyltransferase

Cat.No: T73134

Cat.No: T63970

Cat.No: T64208

Cat.No: T7305

Target: Histone Methyltransferase

Cat.No: T12428L

Target: Histone Methyltransferase

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

CPI-169 racemate

Cat.No: T6809

Synonym: CPI 169,CPI-169,CPI169

Target: Epigenetic Reader Domain, Histone Methyltransferase

Cat.No: T2435

Target: Histone Methyltransferase

Cat.No: T1775

Target: Histone Methyltransferase

Cat.No: T15194

Target: Histone Methyltransferase

Cat.No: T1905

Target: Histone Methyltransferase

Cat.No: T13780

Target: Apoptosis, Histone Methyltransferase

Cat.No: T12430

Target: Histone Methyltransferase

Cat.No: T8510

Synonym: Lirametostat

Target: Histone Methyltransferase

Cat.No: T3057

Target: Histone Methyltransferase, Autophagy

Cat.No: T6059

Target: Histone Methyltransferase, Autophagy

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

3-deazaneplanocin A HCl

Cat.No: T6360

Target: Others, Histone Methyltransferase

Cat.No: T40199

Synonym: CPI-0209

Target: Histone Methyltransferase

Cat.No: T6810

Synonym: Synonym 2,CPI 360,CPI360

Target: Apoptosis, Histone Methyltransferase

Cat.No: T29231

Synonym: ZLD-1039,ZLD 1039

Target: Histone Methyltransferase

Cat.No: T10205

Target: Histone Methyltransferase

PF-06726304 acetate

Cat.No: T12428

Target: Histone Methyltransferase

Tazemetostat trihydrochloride

Cat.No: T15240

Synonym: EPZ-6438 trihydrochloride,E-7438 trihydrochloride

Target: Histone Methyltransferase

Cat.No: T40038

Synonym: UNC2399

Cat.No: T11436

Target: Histone Methyltransferase

Cat.No: T27069

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

Cat.No: T79200

Target: Histone Methyltransferase

Cat.No: T25471

Synonym: GSK A

EPZ011989 HCl(1598383-40-4 Free base)

Cat.No: T2435L

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

Cat.No: T39971

Cat.No: T36799

Cat.No: T69771

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。
TN5096	Tanshindiol B	Histone Methyltransferase	Chromatin/Epigenetic
	Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information for designing a new class of potent EZH2 inhibitors. It also possesses the anti-angiogenic act
TN5097	Tanshindiol C	LDL; Histone Methyltransferase	Chromatin/Epigenetic; Metabolism
	Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for therapeutic intervention of atherosclerosis.It possesses a unique anti-cancer activity whose mechani

天然产物

Gambogenic acid

Cat.No: T8201

Target: Histone Methyltransferase

Cat.No: TN5096

Target: Histone Methyltransferase

Cat.No: TN5097

Target: LDL, Histone Methyltransferase

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