货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S55799-1ml促销	10mM in DMSO	￥720.00 ￥570.00 S55799-1ml ￥570.00 现货	9 9	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S55799-1ml促销

10mM in DMSO

￥720.00 ￥570.00

产品描述：

TEAD 抑制剂;TEAD Inhibitors;;InformationMGH-CP1 MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation . MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.TargetsTEAD4 (Cell-free assay); TEAD2 (Cell-free assay) 672 nM; 710 nMIn vitroMGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro. MGH-CP1 treatment markedly decreases the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 does not affect auto-palmitoylation of several ZDHHC-family palmitoyl acyltransferases, suggesting its selectivity toward TEADs. MGH-CP1 is a selective small-molecule pan-TEAD inhibitor by directly targeting TEAD auto-palmitoylation.In vivoMGH-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.Cell Research(from reference)Cell lines：HEK293T cells, Lats1/2 conditional MEFs, MDA-MB-231 cells, Huh7 cells Concentrations：0.1 μM, 0.3 μM, 0.6 μM, 1 μM, 1.2 μM, 2.5 μM, 3 μM, 5 μM, 10 μM Incubation Time：24 h

靶点：

IC50: 710 nM (TEAD2), 672 nM (TEAD4)

体内研究：

MGH-CP1 (75mg/kg；口服；每日一次，持续 2 周) 可抑制野生型小鼠肠上皮中 TEAD 蛋白的棕榈酰化，但可抑制 Lats1/2 KO 小鼠肠道中 TEAD 靶基因 CTGF 和 ANKRD1 的上调。

参考文献：

1. Li Q, Sun Y, Jarugumilli GK, et al. Lats1/2 Sustain Intestinal Stem Cells and Wnt Activation through TEAD-Dependent and Independent Transcription. Cell Stem Cell. 2020;26(5):675-692.e8. doi:10.1016/j.stem.2020.03.002

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.714 ml	13.569 ml	27.137 ml
5 mM	0.543 ml	2.714 ml	5.427 ml
10 mM	0.271 ml	1.357 ml	2.714 ml
50 mM	0.054 ml	0.271 ml	0.543 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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