Jin, Jia; Ye, Xiaoqing; Boateng, Derrick; Dai, Kaili; Ye, Fei; Du, Pengfei; Yu, Han published the artcile< Identification and characterization of potent and selective inhibitors targeting protein tyrosine phosphatase 1B (PTP1B)>, Safety of 3-(4-Bromophenyl)acrylaldehyde, the main research area is PTP1B type 2 diabetes protein tyrosine phosphatase 1B; Dihydropyridine thione; PTP1B; Selective inhibitors; TCPTP; Type 2 diabetes.
Protein tyrosine phosphatase 1B (PTP1B) plays an important role in the neg. regulation of insulin and leptin signaling. The development of small mol. inhibitors targeting PTP1B has been validated as a potential therapeutic strategy for Type 2 diabetes (T2D). In this work, we have identified a series of compounds containing dihydropyridine thione and particular chiral structure as novel PTP1B inhibitors. Among those, compound 4b(I, CAS 2071719-61-2) showed moderate activity with IC50 value of 3.33 μM and meanwhile with good selectivity (>30-fold) against TCPTP. The further MOA study of PTP1B demonstrated that I is a substrate-competitive inhibitor. The binding mode anal. suggested that I simultaneously occupies the active site and the second phosphotyrosine (pTyr) binding site of PTP1B. Furthermore, the cell viability assay of I showed tolerable cytotoxicity in L02 cells, thus I may be prospectively used to further in vivo study.
Bioorganic & Medicinal Chemistry Letters published new progress about Enzyme kinetics. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Safety of 3-(4-Bromophenyl)acrylaldehyde.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary