MGH-CP1, inhibitor

MGH-CP1

Cat. Num. AAA5765154

• Purity: 0.9976
• Synonyms: MGH-CP1; inhibitor

• Purity/Purification: 0.9976
• Form/Format: Solid

• Solubility: Ethanol: 74mg/mL (200.81mM); DMSO: 74mg/mL (200.81mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• SMILES: C1C2CC3CC1CC(C2)(C3)C4=CC=C(C=C4)NC(=O)CSC5=NC=NN5
• Formula: C20H24N4OS
• 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-beta-Catenin-deltaN90, 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.
• In vitro: 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
• CAS Number: 896657-58-2
• Preparation and Storage: Store at 0-4 degree C for short term (days to weeks), or -20 degree C for long term (months).

Chemical Structure

Related Product Information for MGH-CP1, inhibitor

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 and 672,respectively.

Product Categories/Family for MGH-CP1, inhibitor

Others

References

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.