MGH-CP1 |
| Catalog No.GC66462 |
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.
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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *