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MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s 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 induce apoptosis when together with Lats1/2 deletion. MGH-CP1 potently inhibits TEAD-mediated transcription in a dose-dependent manner and effectively blocks cell over-proliferation.
In vivo, 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.
| Molecular Weight | 368.50 |
| Formula | C20H24N4OS |
| CAS Number | 896657-58-2 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage | 2-8°C, protect from light, dry, sealed |
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