规格

价格

库存

数量

1 mg

¥ 783

现货

2 mg

¥ 1,150

现货

5 mg

¥ 2,290

现货

10 mg

¥ 3,390

现货

25 mg

¥ 5,460

现货

50 mg

¥ 7,430

现货

100 mg

¥ 9,830

现货

1 mL x 10 mM (in DMSO)

¥ 1,650

现货

生物活性

产品描述	SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
靶点活性	CARM1:50 nM
体外活性	除PRMT6（IC50=5.2 μM）外，SGC2085不抑制其他PRMTs。在测试三种不同浓度（1, 10, 和50 μM）的21种人类蛋白质甲基转移酶中，SGC2085显示出完全的选择性。为了表征SGC2085在溶液中的作用机制，于不同浓度的SAM和肽底物下测定IC50值。底物肽或辅因子浓度的增加不影响IC50值，这表明抑制机制为非竞争性，这一点之前已在其他结合于底物口袋的蛋白质甲基转移酶抑制剂上显示过[1]。在HEK293细胞中以10 μM测试高达48小时时，SGC2085未观察到细胞活性，而双重CARM1/PRMT6抑制剂MS049的10 μM则能够阻断BAF155的甲基化。我们假设SGC2085缺乏细胞活性是由于其较差的渗透性[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].

化学信息

分子量	312.41
分子式	C₁₉H₂₄N₂O₂
CAS No.	1821908-48-8
Smiles	C[C@H](N)C(=O)NCc1ccc(Oc2cc(C)cc(C)c2)c(C)c1
密度	1.097 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: 40 mg/mL (128.04 mM), Sonication is recommended.

H2O: Insoluble

DMSO: 55 mg/mL (176.05 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.4 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2009 mL	16.0046 mL	32.0092 mL	160.0461 mL
5 mM	0.6402 mL	3.2009 mL	6.4018 mL	32.0092 mL
10 mM	0.3201 mL	1.6005 mL	3.2009 mL	16.0046 mL
20 mM	0.1600 mL	0.8002 mL	1.6005 mL	8.0023 mL
50 mM	0.0640 mL	0.3201 mL	0.6402 mL	3.2009 mL
100 mM	0.0320 mL	0.1600 mL	0.3201 mL	1.6005 mL