UNC0638

"目录号: HY-15273

EpigeneticsAutophagy-

UNC0638 是一种有效的G9a(EHMT2) (IC50<15 nM) 和GLP(EHMT1) (IC50=19 nM) 抑制剂。

Histone MethyltransferaseAutophagy

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生物活性

Description

UNC0638 is a potentG9a(EHMT2) (IC50<15 nM) andGLP(EHMT1) inhibitor (IC50=19 nM) in S-adenosyl-L-homocysteine hydrolase (SAHH)-coupled assays.

IC50& Target

IC50: <15 nM (G9a), 19±1 nM (GLP)[1]

In Vitro

UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.The Kiof UNC0638 is determined to be 3.0±0.05 nM (n=2). Consistent with this, the Morrison Kifor UNC0638 is 3.7±0.2 nM (n=3). The selectivity of UNC0638 over a wide range of epigenetic targets is evaluated. Notably, UNC0638 is inactive against other H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL and SMYD3), H3K79 (DOT1L) and H4K20 (SETD8) methyltransferases, as well as PRDM1, PRDM10 and PRDM12. In addition, UNC0638 is inactive against protein arginine methyltransferases PRMT1 and PRMT3, and HTATIP, a histone acetyltransferase. Of note, UNC0638 has weak but measurable activity against JMJD2E (IC50=4,500±1,100 nM), a Jumonji protein demethylase and DNA methyltransferase DNMT1 (IC50=107,000±6,000 nM). Nevertheless, the selectivity of UNC0638 for G9a and GLP over JMJD2E is >200-fold, and selectivity for G9a and GLP over DNMT1 is >5,000-fold[1]. UNC0638 is a type of small molecule that can specifically inhibit the enzyme activity of histone methyltransferase EHMT and reduce the H3K9 dimethylation (H3K9me2) levels in cells[2].

References

[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.