GSK2850163

GSK2850163 C화학적 특성, 용도, 생산

Biochem/physiol Actions

GSK2850163 is a highly selective inhibitor of inositol requiring enzyme-1 alpha (IRE1α) with dual activity: it inhibits IRE1α kinase activity with an IC50 value of 20 nM and RNase activity with an IC50 value of 200 nM. IRE1α is a dual serine/threonine-protein kinase/endoribonuclease with two enzymatic domains: a trans-autophosphorylation domain and and endoribonuclease (RNase) domain. When activated, usually in response to endoplasmic reticulum (ER) stress such as the unfolded protein response (UPR), IRE1α oligomerizes and activates mRNA splicing of adaptive XBP1 transcription factor, which upregulates ER chaperones and ER associated degradation (ERAD) genes that promote degradation of ER unfolded proteins and facilitate recovery from ER stress. However, if ER stress is too high or chronic, IRE1α is hyperactivated, increasing many ER mRNAs, resulting in apoptosis. GSK2850163 interacts with IRE1α catalytic residues Lys599 and Glu612, displacing the kinase activation loop to the inactive DFG-out conformation. The rearrangement of the kinase domain-dimer interface also results in the RNAse domains rotating away from each other, inhibiting the RNase activity.

GSK2850163 준비 용품 및 원자재

원자재

준비 용품

GSK2850163 공급 업체

공급자	전화	이메일	국가	제품 수	이점
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	52927	58
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51471	80
ChemeGen(Shanghai) Biotechnology Co.,Ltd.	18818260767	sales@chemegen.com	China	11289	58
Shanghai hongqu biomedical technology co. LTD	88888888888	hongquchem@qq.com	China	5132	58
Chunchuang (Wuhan) Technology Co., Ltd	15342225168	yutianchun2007@126.com	China	10010	58
InvivoChem	13549236410	sales@invivochem.cn	China	6749	58
TargetMol Chemicals Inc.	4008200310	marketing@tsbiochem.com	China	24017	58
Nantong QuanYi Biotechnology Co., Ltd	0513-66337626 18051384581	sales@chemhifuture.com	China	4249	58