| 名称 | MGH-CP1 |
| 描述 | MGH-CP1 is a potent and selective inhibitor of TEAD palmitoylation, demonstrating dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 values of 710 nM and 672 nM, respectively. |
| 细胞实验 | 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. |
| 体外活性 | 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. |
| 体内活性 | 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 |
| 存储条件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 74 mg/mL (200.81 mM)
DMSO : 45 mg/mL (122.12 mM)
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| 关键字 | MGH CP1 | Lats1/2 deletion | Myc | MGHCP1 | TEAD auto-palmitoylation | Apoptosis | Epithelial | inhibit | MGH-CP1 | Inhibitor | MGH-CP-1 |
| 相关库 | 经典已知活性库 | 抑制剂库 | NO PAINS 化合物库 | 口服活性化合物库 | 已知活性化合物库 |
United States
