Home Hippo TEAD inhibitor MGH-CP1 For research use only.

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.

MGH-CP1 Chemical Structure

MGH-CP1 Chemical Structure

CAS No. 896657-58-2

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MGH-CP1 Related Products

Biological Activity

Description 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.
Targets
TEAD4 [1]
(Cell-free assay)		 TEAD2 [1]
(Cell-free assay)
672 nM 710 nM
In vitro
In vitro

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]
Cell Research Cell lines HEK293T cells, Lats1/2 conditional MEFs, MDA-MB-231 cells, Huh7 cells
Concentrations 0.1 μM, 0.3 μM, 0.6 μM, 1 μM, 1.2 μM, 2.5 μM, 3 μM, 5 μM, 10 μM
Incubation Time 24 h
Method

HEK293T cells, Lats1/2 conditional MEFs and MDA-MB-231 cells are cultured in DMEM supplemented with 10% FBS and 1% penicillin/streptomycin. Transfection in HEK293T cells is performed using Lipofectamine 2000. For luciferase reporter assays, HEK293T cells are transfected with the luciferase reporter constructs TBS-Luc, Super TOP-FLASH (STF), Gli-BS-Luc, BRE-Luc, and NF-kB-Luc, as well as the expression vectors of pGIPZ-YAP5SA, pGIPZ-YAP6SA, pGIPZ-TAZ4SA, pLV-b-Catenin-DN90, pCIG-Wnt3a, pCMV-LRP5C, pCIG-BMP4, pCIG-Gli1, pGIPZ-IKBKE and pCMV-Renilla lucifease. Luciferase activities are conducted 24 hours after transfection using the dual-lucif-erase reporter kit in the cells treated with or without Wnt3A, LiCl or MGH-CP1.
In Vivo
In vivo

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]
Animal Research Animal Models wild-type mice, mice carrying Lats1/2 or APC conditional alleles
Dosages 75mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 368.50 Formula

C20H24N4OS
CAS No. 896657-58-2 SDF --
Smiles O=C(CSC1=NN=C[NH]1)NC2=CC=C(C=C2)C34CC5CC(CC(C5)C3)C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 74 mg/mL ( (200.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 74 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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