MGH-CP1

製品コードS9735 バッチS973502

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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. This compound treatment markedly decreases the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. It does not affect auto-palmitoylation of several ZDHHC-family palmitoyl acyltransferases, suggesting its selectivity toward TEADs. This chemical 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. This compound can effectively inhibit the palmitoylation of TEAD proteins in the intestinal epithelium. It 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, this chemical 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. 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 this compound.
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

参考

https://pubmed.ncbi.nlm.nih.gov/32259481/

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：

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

長期の保管のために-20°Cの下で製品を保ってください。

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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