Product Details
| Product Name:
MGH-CP1 |
CAS No.:
896657-58-2 |
| Purity:
98.66% |
Supply Ability:
10g |
| Release date:
2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | 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. |
| 細胞實驗 | 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. |
| 體外活性 | 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. |
| 體內(nèi)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 |
| 存儲條件 | 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)
|
| 關(guān)鍵字 | MGH CP1 | Lats1/2 deletion | Myc | MGHCP1 | TEAD auto-palmitoylation | Apoptosis | Epithelial | inhibit | MGH-CP1 | Inhibitor | MGH-CP-1 |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抑制劑庫 | NO PAINS 化合物庫 | 口服活性化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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