MGH-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.
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包装价格促销价数量
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5mg￥762.00610.00- +
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10mg￥1212.00970.00- +
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25mg￥2612.002090.00- +
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50mg￥4525.003620.00- +
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100mg￥7337.005870.00- +
- 货号: ajcf14652
- CAS: 896657-58-2
- 别名:
- 分子式: C20H24N4OS
- 分子量: 368.5
- 纯度: ＞98%
- 溶解度:
- 储存: 4°C, away from moisture and light
- 库存: 现货
Background
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.
