MGH-CP1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MGH-CP1 是一种有效的选择性 TEAD 棕榈酰化抑制剂。它在体外对 TEAD2/4 自棕榈酰化表现出剂量依赖性和有效抑制作用，IC50 分别为 710 nM 和 672 nM。

MGH-CP1 is a potent and selective inhibitor TEAD palmitoylation. It exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively.

MGH-CP1 (0-100 μM) inhibits auto-palmitoylation of recombinant TEAD2 and TEAD4 in a dose-dependent manner.MGH-CP1 (0-2 μM) inhibits TEAD-binding sites (TBS)-Luc reporter activity in a dose-dependent manner in YAP-expressing HEK293 cells.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.MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion.

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. Animal Model:Mice (induced high-dose Cre recombination by intraperitoneal injection of 120mg/kg Tamoxifen for two consecutive days)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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Others

Other Targets

TEAD|TEAD2|TEAD4

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896657-58-2

368.5

C20H24N4OS

>98% (HPLC)

DMSO:74 mg/mL (200.81 mM);Ethanol:74 mg/mL (200.81 mM)

C1C2CC3CC1CC(C2)(C3)C4=CC=C(C=C4)NC(=O)CSC5=NC=NN5

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(-20℃)

With Ice Pack

≥ 2 years