I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors published in 2019.0. Formula: C7H5NO4, Reprint Addresses Luo, C (corresponding author), Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China.; Zhou, B (corresponding author), Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China.. The CAS is 62-23-7. Through research, I have a further understanding and discovery of 4-Nitrobenzoic acid
Transcriptional enhancer associated domain family members (TEADs) are the most important downstream effectors that play the pivotal role in the development, regeneration and tissue homeostasis. Recent biochemical studies have demonstrated that TEAD5 could undergo autopalmitoylation that is indispensable for its function making the lipid-binding pocket an attractive target for chemical intervention. Herein, through structure-based virtual screen and rational medicinal chemistry optimization, we identified DC-TEADin02 as the most potent, selective, covalent TEAD autopalmitoylation inhibitor with the IC50 value of 197 +/- 19 nM while it showed minimal effect on TEAD-YAP interaction. Further biochemical counter-screens demonstrate the specific thiol reactivity and selectivity of DC-TEADin02 over the kinase family, lipid-binding proteins and epigenetic targets. Notably, DC-TEADin02 inhibited TEADs transcription activity leading to downregulation of YAP-related downstream gene expression. Taken together, our findings proved the validity of modulating transcriptional output in the Hippo signaling pathway through irreversible chemical interventions of TEAD5 autopalmitoylation activity, which may serve as a qualified chemical tool for TEADs palmitoylation-related studies in the future. (C) 2019 Elsevier Masson SAS. All rights reserved.
Welcome to talk about 62-23-7, If you have any questions, you can contact Lu, WC; Wang, J; Li, Y; Tao, HR; Xiong, H; Lian, FL; Gao, J; Ma, HN; Lu, T; Zhang, D; Ye, XQ; Ding, H; Yue, LY; Zhang, YY; Tang, HY; Zhang, NX; Yang, YX; Jiang, HL; Chen, KX; Zhou, B; Luo, C or send Email.. Formula: C7H5NO4
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Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem