MGH-CP1

立即咨询

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。

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 tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation 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.