UNC0638

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Chemical Structure| 1255580-76-7 同义名 : -
CAS号 : 1255580-76-7
货号 : A389386
分子式 : C30H47N5O2
纯度 : 99%+
分子量 : 509.73
MDL号 : MFCD22208587
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(58.86 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

1M HCl: 100 mg/mL(196.18 mM)，配合低频超声，并调节pH至1
动物实验配方：
生物活性
描述 UNC0638 is an inhibitor of G9a and GLP with remarkable potency and selectivity across a wide array of epigenetic and non-epigenetic targets. The Ki value of UNC0638 is determined to be 3.0±0.05 nM (n=2), consistent with the Morrison Ki value of 3.7±0.2 nM (n=3). UNC0638 exhibits notable selectivity over various epigenetic targets, including H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL, and SMYD3), H3K79 (DOT1L), and H4K20 (SETD8) methyltransferases, as well as PRDM1, PRDM10, and PRDM12. Additionally, UNC0638 displays inactivity against protein arginine methyltransferases PRMT1 and PRMT3, and HTATIP, a histone acetyltransferase. Although UNC0638 exhibits weak but detectable activity against JMJD2E (IC50=4,500±1,100 nM), a Jumonji protein demethylase, and DNA methyltransferase DNMT1 (IC50=107,000±6,000 nM), its selectivity for G9a and GLP over JMJD2E exceeds 200-fold, and its selectivity over DNMT1 exceeds 5,000-fold [1]. UNC0638 is a small molecule that selectively inhibits the enzymatic activity of histone methyltransferase EHMT, consequently reducing H3K9 dimethylation (H3K9me2) levels in cells [2].
作用机制 UNC0638 is a substrate-competitive inhibitor, but does not compete with the cofactor SAM, which is distinguished with the other inhibitor. [2]
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
22Rv1 cells Function assay Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay, IC50=0.048 μM 21780790
H1299 cells 0.25 uM Function assay 24 h Inhibition of G9a expressed in H1299 cells assessed as inhibition of dimethylation of p53 at lys 373 at 0.25 uM after 24 hrs by Western blot analysis 21780790
HCT116 cells Function assay Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay, IC50=0.21 μM 21780790
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.81mL

1.96mL

0.98mL

19.62mL

3.92mL

1.96mL
参考文献

[1]Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.

[2]Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5.