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Cat. No.	Product Name	Target	Signaling Pathways
T1841	UNC0379	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0379 是一种选择性的、底物竞争性的赖氨酸甲基转移酶 SETD8 抑制剂，IC50值为 7.3 μM，也选择性抑制其他 15 种甲基转移酶。
T17203	UNC0224	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0224 是 G9a 的特异性抑制剂，Ki 为 2.6 nM，IC50 为 15 nM。 UNC0224 还有效抑制 GLP，IC50 值为 20-58 nM。
T4583	PFI-2 hydrochloride (R)-PFI-2 hydrochloride,PFI-2 HCl	Histone Methyltransferase	Chromatin/Epigenetic
	PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) 是一种有效的、高度选择性的、具有细胞活性的 SETD7 甲基转移酶抑制剂，IC50值为2nM，活性是 (S)-PFI-2 的 500 倍。
T1987	PFI-2 PFI2,PFI 2,(R)-PFI-2	Histone Methyltransferase	Chromatin/Epigenetic
	PFI-2 是一种有效、特异性和细胞活性的赖氨酸甲基转移酶 SETD7 抑制剂，Ki 和 IC50值分别为 0.33 和 2 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。
T14841	BVT948	Phosphatase; P450; Histone Methyltransferase	Chromatin/Epigenetic; Metabolism
	BVT948 是一种蛋白酪氨酸磷酸酶抑制剂，还可以抑制赖氨酸甲基转移酶 SETD8 (KMT5A) 和几种细胞色素 P450 (P450) 同工型。
T6879	LLY-507 LLY507,LLY 507	Histone Methyltransferase	Chromatin/Epigenetic
	LLY-507 是一种有效的、细胞活性的、特异性的蛋白质赖氨酸甲基转移酶 SMYD2 抑制剂。它是一种化学探针，用于解析 SMYD2 在癌症和其他生物过程中的功能。它有抑制 SMYD2 甲基化 p53 肽的能力，IC50小于 15 nM。
TQ0232	UNC0646 UNC 0646	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0646 是一种有效的、选择性的同源蛋白赖氨酸甲基转移酶 G9a 和 GLP 抑制剂，IC50分别为 6 和 15 nM，对 G9a/GLP 的选择性比 SETD7、SUV39H2、SETD8 和 PRMT3 高。它降低 MDA-MB-231 细胞中H3K9me2的水平，IC50为 26 nM。
T25471	GSK-A GSK A
	GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor.
T10553	BIX-01338 hydrate	Others	Others
	BIX-01338 hydrate is an inhibitor of histone lysine methyltransferase.
T28111	MS012 MS-012,MS 012
	MS012 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase (Kd = 46 ± 15 nM).
T36799	UNC 2399
	Biotinylated UNC 1999 (Cat.No. 4904, IC50 = 17 nM). Enriches lysine methyltransferase EZH2 from HEK293T cells. Negative control also avilable. 0
T40993	Histone H3 (1-21) Histone H3 (1-21)
	Histone H3 (1-21) is a truncated form of the Histone H3 protein consisting of amino acids 1 to 21. It serves as a common substrate for methyltransferase assays targeting Histone 3 at lysine 4 and lysine 9, as well as for acetyltransferase assays targeting Histone 3 at lysine 9 and lysine 14.
T69624	TC-5115
	TC-5115 is a potent inhibitor of MLL methyltransferase with IC50 value of 16 nM. TC-5115 may lead to the development of a new therapy for the treatment of human MLL leukemia. The mixed-lineage leukemia (MLL) protein, also known as MLL1, is a lysine methyltransferase specifically responsible for methylation of histone 3 lysine 4. MLL has been pursued as an attractive therapeutic target for the treatment of acute leukemia carrying the MLL fusion gene or MLL leukemia.
T11185	EML741	Histone Methyltransferase	Chromatin/Epigenetic
	EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.
T81175	SETD7-IN-1	Histone Methyltransferase	Chromatin/Epigenetic
	SETD7-IN-1 (compound 7) 为 PFI-2 类似物，兼具组蛋白赖氨酸甲基转移酶SETD7的底物与抑制剂功能，展现出 0.96±0.10 µM 的 IC50 值。
T22250	5WKS ZINC97756584	Others	Others
	5WKS 也称为ZINC97756584，是一种生物化学物质。它是G9a 蛋白抑制剂。G9A/EHMT2是一种核组蛋白赖氨酸甲基转移酶，催化H3K9me2，这是一种通常与转录基因沉默相关的可逆修饰。5WKS 可用于自身免疫性疾病或肿瘤的研究。
T63705	UNC0379 TFA
	UNC0379 TFA 是选择性的、底物竞争性的赖氨酸甲基转移酶 SETD8(KMT5A) 抑制剂 (IC50: 7.3 μM)，对其他 15 种甲基转移酶表现出良好的选择性。
T28114	MS2177 MS 2177,MS-2177
	MS2177 is a potent and selective inhibitor of SETD8, the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). MS2177 has an in vitro IC50 of 1.9 μM (σ = 1.05 μM, n = 4) in ascintillation proximity assay. Binding of MS2
T26744	BAY-598 R-isomer BAY598 R-isomer,BAY 598 R-isomer
	BAY-598 R-异构体是BAY589的R-异构体，它可用作参考化合物。它是是赖氨酸N-甲基转移酶（SMYD2）的抑制剂，对SMYD2比蛋白酶激活的受体1（PAR1）具有选择性。
T36802	Bisubstrate Inhibitor 78
	Bisubstrate inhibitor 78 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50= 1.41 μM).1It binds the NNMT active site in the binding pockets for the NNMT substrates S-adenosyl-L-methionine (SAM) and nicotinamide . Bisubstrate inhibitor 78 is selective for NNMT over histone-lysine N-methytransferase NSD2 and protein arginine methyltransferase 1 (PRMT1; IC50s = >50 μM for both). It reduces levels of 1-methylnicotinamide in, and inhibits proliferation of, HSC-2 oral cancer cells when us...
T36576	Histone H3 (21-44)-GK-biotin (trifluoroacetate salt) Histone H3 (21-44)-GK-biotin (trifluoroacetate salt)
	Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.1 and 3.2 sequences and is biotinylated via a C-terminal GK linker. Histone H3 (21-44) contains a lysine residue at position 23 that is subject to acetylation, an arginine at position 26 subject to methylation, and a serine at position 28 subject to phosphorylation, as well as lysine residues at positions 27 and 36 that are subject to methylation and acetylation....
T35567	BIX01294 (hydrochloride hydrate)
	The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other ...
T79776	ZZM-1220	Histone Methyltransferase	Chromatin/Epigenetic
	ZZM-1220是一种针对组蛋白赖氨酸甲基转移酶G9a/GLP的共价抑制剂，IC50值分别为458 nM和924 nM。该化合物能有效抑制H3K9me2在细胞中的作用，从而显著促进三阴性乳腺癌(TNBC)细胞的凋亡(apoptosis)，同时在G2/M期阻断细胞周期的进程。
T73225	OTS193320
	OTS193320 是一种咪唑并 [1,2-a] 吡啶化合物，一种 SUV39H2甲基转移酶活性抑制剂。OTS193320 降低乳腺癌细胞中的全局组蛋白 H3 赖氨酸 9 三甲基化水平并引发凋亡细胞死亡。与单一药剂 OTS193320 或 DOX 相比，OTS193320 与 Doxorubicin(DOX) 的组合可以导致 γ-H2AX 水平以及癌细胞活力的降低。
T83755	ssK36 TFA
	ssK36是一种针对组蛋白甲基转移酶SET结构域含蛋白2 (SETD2) 的肽类超级底物，其对应于组蛋白H3赖氨酸36 (H3K36) 的第29至43个氨基酸，且在第31、32、36、37和39位氨基酸上发生了置换。在无细胞检测中，ssK36的甲基化程度比H3K36 (29-43) 高70倍，速度快290倍。
T83867	UNC8153 TFA
	UNC8153 是一种 NSD2（组蛋白-赖氨酸 N-甲基转移酶）的降解剂，其通过诱导NSD2的降解，具有350 nM的50%降解常数（DC50）值，并且在20 µM浓度下对NSD2具有选择性，而不选择NSD1和NSD3。在MM.1S多发性骨髓瘤细胞中，UNC8153 (10 µM) 能够诱导NSD2降解并减少组蛋白H3赖氨酸36位二甲基化（H3K36me2），这一效应可以被泛素激活酶抑制剂MLN4924所抑制。它减少了表达带有在1099位上谷氨酸到赖氨酸激活突变的NSD2（NSD2E1099K）的MM.1S细胞的增殖，但在20 µM浓度下，对表达野生型NSD2的MDA-MB-231、U2OS或HEK293细胞无效。UNC8153 (20 µM) 降低了在迁移实验中MM.1S细胞的附着能力。

化合物

Cat.No: T1841

Target: Histone Methyltransferase

Cat.No: T17203

Target: Histone Methyltransferase

PFI-2 hydrochloride

Cat.No: T4583

Synonym: (R)-PFI-2 hydrochloride,PFI-2 HCl

Target: Histone Methyltransferase

Cat.No: T1987

Synonym: PFI2,PFI 2,(R)-PFI-2

Target: Histone Methyltransferase

Cat.No: T7305

Target: Histone Methyltransferase

Cat.No: T14841

Target: Phosphatase, P450, Histone Methyltransferase

Cat.No: T6879

Synonym: LLY507,LLY 507

Target: Histone Methyltransferase

Cat.No: TQ0232

Synonym: UNC 0646

Target: Histone Methyltransferase

Cat.No: T25471

Synonym: GSK A

BIX-01338 hydrate

Cat.No: T10553

Target: Others

Cat.No: T28111

Synonym: MS-012,MS 012

Cat.No: T36799

Histone H3 (1-21)

Cat.No: T40993

Synonym: Histone H3 (1-21)

Cat.No: T69624

Cat.No: T11185

Target: Histone Methyltransferase

Cat.No: T81175

Target: Histone Methyltransferase

Cat.No: T22250

Synonym: ZINC97756584

Target: Others

Cat.No: T63705

Cat.No: T28114

Synonym: MS 2177,MS-2177

BAY-598 R-isomer

Cat.No: T26744

Synonym: BAY598 R-isomer,BAY 598 R-isomer

Bisubstrate Inhibitor 78

Cat.No: T36802

Histone H3 (21-44)-GK-biotin (trifluoroacetate salt)

Cat.No: T36576

Synonym: Histone H3 (21-44)-GK-biotin (trifluoroacetate salt)

BIX01294 (hydrochloride hydrate)

Cat.No: T35567

Cat.No: T79776

Target: Histone Methyltransferase

Cat.No: T73225

Cat.No: T83755

Cat.No: T83867

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