lysine methyltransferase

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。

DCG066 是一种赖氨酸甲基转移酶 G9a 的抑制剂，具有抗癌活性，通过 Nrf2 HO-1 通路抑制 MM 细胞的增殖并诱导铁死亡，可用于研究白血病。

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 used at a concentration of 100 μM.This compound is unstable in powder form and other related salt forms are recommended.

lutidinic acid (2,4-Dicarboxypyridine) 是一种体外和细胞内抑制剂，也是一种已知的组蛋白赖氨酸脱甲基酶抑制剂。

BIX-01338 hydrate is an inhibitor of histone lysine methyltransferase.

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.

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。

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。

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。

Menin–KMT2A-IN-1 (Compound 20) 是一种具有高效抑制性的menin–KMT2A抑制剂，可与menin结合，其IC50为8 nM，并阻止menin与赖氨酸甲基转移酶2A (KMT2A) 的相互作用。该化合物对hERG的抑制作用的IC50为65 μM，对MV4-11细胞的IC50为74 nM。在CD-1小鼠中，Menin–KMT2A-IN-1展示出良好的药代动力学性能，口服生物利用度达到74%。

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。

GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor.

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。

MS012 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase (Kd = 46 ± 15 nM).

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

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 known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.

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. Histone H3 (21-44)-GK-biotin has been used as a substrate for the primate-specific histone methyltransferase PR domain-containing protein 7 (PRDM7) to determine substrate specificity.

Biotinylated UNC 1999 (Cat.No. 4904, IC50 = 17 nM). Enriches lysine methyltransferase EZH2 from HEK293T cells. Negative control also avilable. 0

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.

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。

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。

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。

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.

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。