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MGH-CP1

Catalog No. T9032 CAS 896657-58-2

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.

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MGH-CP1, CAS 896657-58-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 347.00
100 mg	In stock	$ 563.00
500 mg	In stock	$ 1,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 87.00

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Purity: 99.76%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	TEAD2:672 nM, TEAD4:710 nM
In vitro	MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro, with IC50 of 710 nM and 672 nM, respectively.?Furthermore, ?MGH-CP1 treatment markedly decreased the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells.
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
Cell Research	HEK293T cells, Lats1/2 conditional MEFs and MDA-MB-231 cells were cultured in DMEM supplemented with 10% FBS and 1% penicillin/streptomycin.?For Lats1/2 conditional MEFs carrying CMV-CreER, Lats1/2 was deleted by incubation with 4-OH Tamoxifen (2.5 mM) in DMEM for 4 days prior to further experiment.?Transfection in HEK293T cells was performed using Lipofectamine 2000 (Invitrogen).?For luciferase reporter assays, HEK293T cells were transfected with the luciferase reporter constructs TBS-Luc (8XGTIIC-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-β-Catenin-ΔN90, pCIG-Wnt3a, pCMV-LRP5C, pCIG-BMP4, pCIG-Gli1,?pGIPZ-IKBKE (Rajurkar et al., 2017) and pCMV-Renilla lucifease.?Luciferase activities were conducted 24 hours after transfection using the dual-luciferase reporter kit (Promega) in the cells treated with or without Wnt3A, LiCl or MGH-CP1.?Assays were conducted in triplicates and quantified using PerkinElmer EnVision plate reader.

Molecular Weight	368.5
Formula	C20H24N4OS
CAS No.	896657-58-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 74 mg/mL (200.81 mM)

DMSO: 74 mg/mL (200.81 mM)

References and Literature

1. Li Q , Sun Y , Jarugumilli G K , et al. Lats1/2 Sustain Intestinal Stem Cells and Wnt Activation through TEAD-Dependent and Independent Transcription[J]. Cell stem cell, 2020.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Orally Active Compound Library NO PAINS Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MGH-CP1 896657-58-2 Others MGH CP1 Lats1/2 deletion Myc MGHCP1 TEAD auto-palmitoylation Apoptosis Epithelial inhibit Inhibitor MGH-CP-1 inhibitor

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