"目录号: HY-13980

GPCR/G ProteinEpigenetics-

UNC0642是有效地选择性的G9a/GLP抑制剂，抑制G9a的IC50值小于2.5 nM。

Sigma ReceptorHistone Methyltransferase

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生物活性

Description

UNC0642 is a potent and selectiveG9a/GLPinhibitor, inhibits G9a/GLP with anIC50of less than 2.5 nM.

IC50& Target

IC50: less than 2.5 nM (G9a, GLP)[1]

In Vitro

UNC0642 displays highin vitroand cellular potency, low cell toxicity, and excellent selectivity. UNC0642 is competitive with the peptide substrate and non-competitive with the cofactor SAM. The Kiof UNC0642 is determined to be 3.7±1 nM. UNC0642 displays highin vitropotency for GLP (IC50< 2.5 nM), similar to G9a. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. UNC0642 exhibits high potency at reducing the H3K9me2 mark, low cell toxicity, and good separation of functional potency and cell toxicity in a number of cell lines. It reduces clonogenicity in PANC-1 cells, a pancreatic carcinoma cell line[1].

In Vivo

A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642results in a plasma Cmax(maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL[1].

References

[1].Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-8942.