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DC-PGKI

Cat.No.:HY-177944

CASNo.:2829198-49-2

分⼦式:C₂₆H₂₉Cl₂N₇O₃

分⼦量:558.46

作⽤靶点:PhosphoglycerateKinase(PGK);Keap1-Nrf2;Interleukin

Related

作⽤通路:MetabolicEnzyme/Protease;NF-κB;Immunology/Inflammation

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性DC-PGKI是⼀种⼝服有效的ATP竞争性PGK1抑制剂(IC50=0.16μM，Kd=99.08nM)。DC-PGKI在体外和

体内均能稳定PGK1，并抑制糖酵解活性和PGK1的激酶功能。DC-PGKI介导的PGK1抑制导致NRF2(核因⼦-

红细胞因⼦2相关因⼦2，NFE2L2)的积累，NRF2随后转位⾄细胞核，与IL-1β和IL-6基因的近端区域结合

，并抑制LPS诱导的这些基因的表达。DC-PGKI可⽤于结肠炎的研究[1]。

IC50TargetPGK1PGK1IL-6IL-1β

0.16μM(IC50)99.08nM(Kd)

体外研究DC-PGKI(0.1-30μM,3h)canincreaseRAW264.7cellsPGK1thermalstabilityinaconcentration-

dependentmanner[1].

DC-PGKI(5-10μM,10h)inhibitsPGK1glycolyticmetabolicactivityintherestingandactivatedinRAW264.7

cells[1].

DC-PGKI(10-20μM)notablydecreasestheSer30phosphorylationlevelofBeclin1inRAW246.7