MGH-CP1

Catalog No.S9735 Batch:S973501

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Technical Data

Formula

C20H24N4OS
Molecular Weight 368.50 CAS No. 896657-58-2
Solubility (25°C)* In vitro DMSO 74 mg/mL (200.81 mM)
Ethanol 74 mg/mL (200.81 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
7.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    wild-type mice, mice carrying Lats1/2 or APC conditional alleles

  • Dosages

    75mg/kg

  • Administration

    Oral gavage

Selleck's MGH-CP1 has been cited by 5 publications

Retinoic acid-induced protein 14 links mechanical forces to Hippo signaling [ EMBO Rep, 2024, 25(9):4033-4061] PubMed: 39160347
TEAD4 is a master regulator of high-risk nasopharyngeal carcinoma [ Sci Adv, 2023, 9(1):eadd0960] PubMed: 36608137
Transcriptional and epigenomic profiling identifies YAP signaling as a key regulator of intestinal epithelium maturation [ Sci Adv, 2023, 9(28):eadf9460] PubMed: 37436997
Transcriptional and epigenomic profiling identifies YAP signaling as a key regulator of intestinal epithelium maturation [ Sci Adv, 2023, 9(28):eadf9460] PubMed: 37436997
Targeting the Hippo/YAP/TAZ signalling pathway: Novel opportunities for therapeutic interventions into skin cancers [ Exp Dermatol, 2022, 31(10):1477-1499] PubMed: 35913427

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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