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MGH-CP1
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。
MGH-CP1图片
CAS NO:896657-58-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MGH-CP1 是一种有效且具有口服活性的 TEAD2 和 TEAD4 自棕榈酰化抑制剂, IC50 分别为 710 nM 和 672 nM。MGH-CP1 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,可抑制 Myc 表达,抑制上皮细胞过度增殖,诱导细胞凋亡 (apoptosis)。
Cas No.896657-58-2
分子式C20H24N4OS
分子量368.5
储存条件4°C, away from moisture and light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MGH-CP1 is a potent and orally activeTEAD2andTEAD4auto-palmitoylation inhibitor withIC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induceapoptosiswhen together with Lats1/2 deletion[1].

MGH-CP1 (0-100 μM) inhibits auto-palmitoylation of recombinant TEAD2 and TEAD4 in a dose-dependent manner[1].
MGH-CP1 (0-2 μM) inhibits TEAD-binding sites (TBS)-Luc reporter activity in a dose-dependent manner in YAP-expressing HEK293 cells[1].
MGH-CP1 does not affect YAP nuclear localization or protein levels but potently inhibits TEAD-mediated transcription in a dose-dependent manner and effectively blocks cell over-proliferation[1].
MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion[1].

MGH-CP1 (75mg/kg; PO; daily, for 2 weeks) inhibits the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine[1].

Animal Model:Mice (induced high-dose Cre recombination by intraperitoneal injection of 120mg/kg Tamoxifen for two consecutive days)[1]
Dosage:75 mg/kg
Administration:PO; daily, for 2 weeks
Result:Effectively inhibited the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but effectively inhibited upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine.