Recently I am researching about NONCOVALENT; APOPTOSIS; PATHWAY; POTENT, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81872731, 21977006, 21807006]. Recommanded Product: Pyrazine-2-carboxylic acid. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid
A series of tripeptidic proteasome inhibitors with furylketone as C-terminus were designed and synthesized. Biochemical evaluations against beta 1, beta 2 and beta 5 subunits revealed that they acted selectively on beta 5 subunit with IC(50)s against chymotrypsin-like (CT-L) activity in micromolar range. LC-MS/MS analysis of the ligand-20S proteasome mixture showed that the most potent compound 11m (IC50 = 0.18 mu M) made no covalent modification on 20S proteasome. However, it was identified acting in a slowly reversible manner in wash-out assay and the reversibility was much lower than that of MG132, suggesting the possibility of these tripeptidic furylketones forming reversible covalent bonds with 20S proteasome. Several compounds were selected for anti-proliferative assay towards multiple cancer cell lines, and compound 11m displayed comparable potency to positive control (MG132) in all cell lines tested. Furthermore, the pharmacokinetic (PK) data in rats indicated 11m behaved similarly (C-max, 2007 mu g/L; AUC(0-t), 680 mu g/L.h; V-ss, 0.66 L/kg) to the clinical used agent carfilzomib. All these data suggest 11m is a good lead compound to be developed to novel anti-tumor agent. (c) 2020 Elsevier Masson SAS. All rights reserved.
Recommanded Product: Pyrazine-2-carboxylic acid. About Pyrazine-2-carboxylic acid, If you have any questions, you can contact Sun, Q; Zhou, TL; Xi, DD; Li, XN; Lu, ZR; Xu, FR; Wang, C; Niu, Y; Xu, P or concate me.
Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem