MGH-CP1

製品コードS9735 バッチS973502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 4°C, away from moisture and light.
化学式

C20H24N4OS
分子量 368.50 CAS No. 896657-58-2
Solubility (25°C)* 体外 DMSO 74 mg/mL (200.81 mM)
Ethanol 18 mg/mL (48.84 mM)
Water Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK293T cells, Lats1/2 conditional MEFs, MDA-MB-231 cells, Huh7 cells
濃度 0.1 μM, 0.3 μM, 0.6 μM, 1 μM, 1.2 μM, 2.5 μM, 3 μM, 5 μM, 10 μM
反応時間 24 h
実験の流れ

HEK293T cells, Lats1/2 conditional MEFs and MDA-MB-231 cells are cultured in DMEM supplemented with 10% FBS and 1% penicillin/streptomycin. For Lats1/2 conditional MEFs carrying CMV-CreER, Lats1/2 is deleted by incubation with 4-OH Tamoxifen (2.5 mM) in DMEM for 4 days prior to further experiment. 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.
動物実験 動物モデル wild-type mice, mice carrying Lats1/2 or APC conditional alleles
投薬量 75mg/kg
投与方法 Oral gavage

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
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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人間や獣医の診断であるか治療的な使用のためにでない。

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