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ML-265 HCl(TEPP-46)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML-265 HCl(TEPP-46)图片
CAS NO:1221186-53-3
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍

TEPP-46 HCl (ML-265) is a novel potent and selective small molecule activator of pyruvate kinase M2 (PKM2) with an EC50 of 92 nM, it showed little or no effect on PKM1, PKL and PKR. Macrophages activated by the TLR4 agonist LPS undergo dramatic changes in their metabolic activity. LPS induces expression of the key metabolic regulator Pyruvate Kinase M2 (PKM2). Activation of PKM2 using the well-characterized small molecules, TEPP-46, inhibited LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. Activation of PKM2 attenuated an LPS-induced proinflammatory M1 macrophage phenotype while promoting traits typical of an M2 macrophage. LPS-induced PKM2 enters into a complex with Hif-1α, which can directly bind to the IL-1β promoter, an event that is inhibited by activation of PKM2. TEPP-46 inhibited LPS-induced glycolytic reprogramming and succinate production. Finally, activation of PKM2 by TEPP-46 in vivo inhibited LPS and Salmonella typhimurium-induced IL-1β production, while boosting production of IL-10. PKM2 is therefore a critical determinant of macrophage activation by LPS, promoting the inflammatory response.

纯度:≥98%

CAS:1221186-53-3 (free base)