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MGH-CP1 Sale

目录号 : GC66462

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.

MGH-CP1 Chemical Structure

Cas No.:896657-58-2

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5mg
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25mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Description

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.

MGH-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.[1]

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.[1]

[1] Qi Li, et al. Cell Stem Cell. 2020 May 7;26(5):675-692.e8.

化学性质

Cas No. 896657-58-2 SDF Download SDF
分子式 C20H24N4OS 分子量 368.5
溶解度 储存条件 4°C, away from moisture and light
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1 mg 5 mg 10 mg
1 mM 2.7137 mL 13.5685 mL 27.137 mL
5 mM 0.5427 mL 2.7137 mL 5.4274 mL
10 mM 0.2714 mL 1.3569 mL 2.7137 mL
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