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17

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T3458	EED226	Histone Methyltransferase	Chromatin/Epigenetic
	EED226 是多梳抑制复合物 2 抑制剂，是一种有效的、选择性的、可口服的胚胎外胚层发育 (EED) 抑制剂，IC50 为 22 nM，具有强抗肿瘤活性。当 H3K27me0 肽用作体外酶法测定的底物时，它抑制 PRC2的 IC50为 23.4 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。
T7378	BRD9539	Histone Methyltransferase	Chromatin/Epigenetic
	BRD9539 是一种组蛋白甲基转移酶G9a 抑制剂，IC50为 6.3 μM，还抑制PRC2活性。
T13954	UNC6852	Histone Methyltransferase; Ligands for Target Protein for PROTAC	Chromatin/Epigenetic; PROTAC
	UNC6852 包含一个 EED 配体 (IC50 = 247 nM) 和一个 von Hippel-Lindau 配体，是一种基于 PROTAC 的特异性多梳抑制复合物 2 (PRC2) 降解剂。
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。
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。
T60044	SPEN-IN-1	Others	Others
	SPEN-IN-1 结合抑制组蛋白 H3K27 三甲基化并阻断 X 染色体失活的起始。 SPEN-IN-1 结合减少了 RepA 的构象空间并取代了同源相互作用的蛋白质因子，包括 PRC2 和 SPEN。
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。
T61825	EED ligand 1
	EED ligand 1 is a highly versatile, potent, and effective inhibitor that specifically targets the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
T17931	EED226-COOH	Others	Others
	EED226-COOH, derived from EED226, serves as a ligand targeting the EED protein for PROTAC applications. It attaches to a VHL ligand through a linker, culminating in the formation of UNC6852, which specifically degrades PRC2[1].
T12554	PROTAC EED degrader-2	Others	Others
	PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27),is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.11.
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。
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
T17653	Boc-NH-C4-acid Boc-5-氨基戊酸	Others; PROTAC Linker	Others; PROTAC
	Boc-NH-C4-acid 是一种属于 Alkyl/ether 类的 PROTAC linker，可用于 PROTAC1 的合成，并且可以降解 PRC2 中的 EED，EZH2，和 SUZ12。
T12553	PROTAC EED degrader-1	Others	Others
	PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.
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: T3458

Target: Histone Methyltransferase

Cat.No: T7305

Target: Histone Methyltransferase

Cat.No: T7378

Target: Histone Methyltransferase

Cat.No: T13954

Target: Histone Methyltransferase, Ligands for Target Protein for PROTAC

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: T10205

Target: Histone Methyltransferase

Cat.No: T60044

Target: Others

Cat.No: T29231

Synonym: ZLD-1039,ZLD 1039

Target: Histone Methyltransferase

Cat.No: T61825

Cat.No: T17931

Target: Others

PROTAC EED degrader-2

Cat.No: T12554

Target: Others

Cat.No: T73134

Tazemetostat trihydrochloride

Cat.No: T15240

Synonym: EPZ-6438 trihydrochloride,E-7438 trihydrochloride

Target: Histone Methyltransferase

Cat.No: T17653

Synonym: Boc-5-氨基戊酸

Target: Others, PROTAC Linker

PROTAC EED degrader-1

Cat.No: T12553

Target: Others

Cat.No: T69771

Cat. No.	Product Name	Target	Signaling Pathways
TN2646	16-Hydroxycleroda-3,13-dien-15,16-olide	Autophagy	Autophagy
	16-Hydroxycleroda-3,13-dien-15,16-olide, and prodigiosin are presented as candidates for autophagy inducers that can trigger cell death in a supplement or alternative medicine for cancer therapy. 16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expre

天然产物

16-Hydroxycleroda-3,13-dien-15,16-olide

Cat.No: TN2646

Target: Autophagy

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