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SGC2085
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SGC2085图片
CAS NO:1821908-48-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议

产品介绍
SGC2085是一种高效选择性CARM1抑制剂,IC50值为50 nM。

产品描述

SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).

体外活性

With the exception of PRMT6 (IC50=5.2 μM), SGC2085 does not inhibit other PRMTs. SGC2085 also shows complete selectivity against a panel of 21 human protein methyltrans- ferases tested at three different concentrations (1,10, and 50 μM). To characterize the mechanism of action of SGC2085 in solution, IC50 values are determined at various concentrations of SAM and peptide substrate. Increasing concentration of substrate peptide or cofactor does not affect IC50 values, indicative of a noncompetitive mechanism of inhibition, which has been previously shown for other protein methyltransferase inhibitors binding at the substrate pocket[1]. No cellular activity is observed for SGC2085 when tested up to 10 μM (48 h exposure in HEK293 cells), while methylation of BAF155 is abrogated by 10 μM of the dual CARM1/PRMT6 inhibitor MS049. We assume that the absence of cellular activity for SGC2085 is due to poor permeability[1].

细胞实验

SGC2085 is dissolved in DMSO and diluted with the appropriate medium before use. HEK293 cells are grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL). Thirty per cent confluent cells are treated with inhibitors or DMSO. After 48 h, media are removed and cells are lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8.0, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% Triton X-100, 12.5 U/mL benzonase), complete EDTA-free protease inhibitor cocktail. After 3 min incubation at room temperature, SDS is added to 1% final concentration. Lysates are run on SDS-PAGE, and immunoblotting is done as outlined below to determine the levels of unmethylated and methylated BAF155[1].

Cas No.

1821908-48-8

分子式

C19H24N2O2

分子量

312.413

储存和溶解度

DMSO:50 mg/mL
Ethanol:40 mg/mL
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years