MGH-CP1 |
| Catalog No.GC66462 |
MGH-CP1 est un inhibiteur d'auto-palmitoylation TEAD2 et TEAD4 puissant et actif par voie orale avec des IC50 de 710 nM et 672 nM, respectivement. MGH-CP1 peut diminuer les niveaux de palmitoylation des protéines TEAD endogènes ou exprimées de manière ectopique dans les cellules. MGH-CP1 peut supprimer l'expression de Myc, inhiber la surprolifération épithéliale et induire l'apoptose lorsqu'il est associé À la suppression de Lats1/2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 896657-58-2
Sample solution is provided at 25 µL, 10mM.
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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[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. |
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