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MGH-CP1

产品编号 T9032 CAS 896657-58-2

MGH-CP1 是 TEAD2 (IC50:710 nM) 及 TEAD4 (IC50:672 nM) 自棕榈酰化抑制剂，口服有活性，可降低细胞内源性或异位表达的 TEAD 蛋白棕榈酰化水平。MGH-CP1 与 Lats1/2 缺失，是 Myc 的表达受到抑制，阻碍上皮细胞过度增殖，诱导细胞凋亡。

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MGH-CP1, CAS 896657-58-2

规格	价格/CNY	货期
1 mg	￥ 262	现货
2 mg	￥ 369	现货
5 mg	￥ 578	现货
10 mg	￥ 913	现货
25 mg	￥ 1,930	现货
50 mg	￥ 2,970	现货
100 mg	￥ 4,380	现货
500 mg	￥ 9,170	现货
1 mL * 10 mM (in DMSO)	￥ 658	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	MGH-CP1 is a potent and selective inhibitor TEAD palmitoylation. It exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.
靶点活性	TEAD2:672 nM, TEAD4:710 nM
体外活性	MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro, with IC50 of 710 nM and 672 nM, respectively.?Furthermore, ?MGH-CP1 treatment markedly decreased the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells.
体内活性	MGH-CP1 inhibits TEAD activity in Lats1/2 KO intestine in vivo. MGH-CP1 can effectively inhibit the palmitoylation of TEAD proteins in the intestinal epithelium. MGH-CP1 is well tolerated and has no apparent adverse effect on overall animal health or body weight after 2 weeks of treatment. In contrast to its lack of apparent effect in wild-type intestine, MGH-CP1 treatment effectively inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO intestine
细胞实验	HEK293T cells, Lats1/2 conditional MEFs and MDA-MB-231 cells were cultured in DMEM supplemented with 10% FBS and 1% penicillin/streptomycin.?For Lats1/2 conditional MEFs carrying CMV-CreER, Lats1/2 was deleted by incubation with 4-OH Tamoxifen (2.5 mM) in DMEM for 4 days prior to further experiment.?Transfection in HEK293T cells was performed using Lipofectamine 2000 (Invitrogen).?For luciferase reporter assays, HEK293T cells were transfected with the luciferase reporter constructs TBS-Luc (8XGTIIC-Luc), Super TOP-FLASH (STF), Gli-BS-Luc, BRE-Luc, and NF-kB-Luc, as well as the expression vectors of pGIPZ-YAP5SA, pGIPZ-YAP6SA, pGIPZ-TAZ4SA, pLV-β-Catenin-ΔN90, pCIG-Wnt3a, pCMV-LRP5C, pCIG-BMP4, pCIG-Gli1,?pGIPZ-IKBKE (Rajurkar et al., 2017) and pCMV-Renilla lucifease.?Luciferase activities were conducted 24 hours after transfection using the dual-luciferase reporter kit (Promega) in the cells treated with or without Wnt3A, LiCl or MGH-CP1.?Assays were conducted in triplicates and quantified using PerkinElmer EnVision plate reader.

分子量	368.5
分子式	C20H24N4OS
CAS No.	896657-58-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 74 mg/mL (200.81 mM)

DMSO: 74 mg/mL (200.81 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.7137 mL	13.5685 mL	27.137 mL	67.8426 mL
	5 mM	0.5427 mL	2.7137 mL	5.4274 mL	13.5685 mL
	10 mM	0.2714 mL	1.3569 mL	2.7137 mL	6.7843 mL
	20 mM	0.1357 mL	0.6784 mL	1.3569 mL	3.3921 mL
	50 mM	0.0543 mL	0.2714 mL	0.5427 mL	1.3569 mL
	100 mM	0.0271 mL	0.1357 mL	0.2714 mL	0.6784 mL

计算器

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分子量计算器

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参考文献

1. Li Q , Sun Y , Jarugumilli G K , et al. Lats1/2 Sustain Intestinal Stem Cells and Wnt Activation through TEAD-Dependent and Independent Transcription[J]. Cell stem cell, 2020.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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