2095304-61-1
Chemical Structure
KH176m
- CAS No.: 2095304-61-1
- Formula:C19H28N2O4
- Molecular Weight:348.44
IUPAC Name: (S)-2-hydroxy-2-methyl-N-((R)-piperidin-3-yl)-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dien-1-yl)butanamide
InChIKey: LEKUGUATSGETDB-KUHUBIRLSA-N
SMILES: C(C[C@](C(N[C@@H]1CCCNC1)=O)(C)O)C2=C(C)C(=O)C(C)=C(C)C2=O
Biological Activity: KH176m is the major active metabolite of KH176 (HY-121577). KH176m is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor that can cross the blood-brain barrier, with an IC50 of 0.16 µM against mouse mPGES-1 and 1.51 µM against human mPGES-1. KH176m blocks LPS- or IL-1β-induced PGE2 production, scavenges ROS, inhibits lipid peroxidation, accelerates NADPH consumption, suppresses the growth of prostate cancer spheroids, reduces the CD44+ CD24− prostate cancer stem cell population, and protects fibroblasts with oxidative phosphorylation defects from redox stress-induced death. KH176m can be used in research related to mitochondrial diseases, inflammatory pain, inflammatory neurological diseases, inflammatory cancers, and prostate cancer[1][2][3].
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KH176m | KH176m is the major active metabolite of KH176 (HY-121577). KH176m is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor that can cross the blood-brain barrier, with an IC50 of 0.16 µM against mouse mPGES-1 and 1.51 µM against human mPGES-1. KH176m blocks LPS- or IL-1β-induced PGE2 production, scavenges ROS, inhibits lipid peroxidation, accelerates NADPH consumption, suppresses the growth of prostate cancer spheroids, reduces the CD44+ CD24− prostate cancer stem cell population, and protects fibroblasts with oxidative phosphorylation defects from redox stress-induced death. KH176m can be used in research related to mitochondrial diseases, inflammatory pain, inflammatory neurological diseases, inflammatory cancers, and prostate cancer. | |||||||||||||||||||||
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References
- [1]. Jiang X, et al. Mechanism of action and potential applications of selective inhibition of microsomal prostaglandin E synthase-1-mediated PGE2 biosynthesis by sonlicromanol's metabolite KH176m. Sci Rep. 2021 Jan 13;11(1):880. [Content Brief]
- [2]. Jiang X, et al. Sonlicromanol's active metabolite KH176m normalizes prostate cancer stem cell mPGES-1 overexpression and inhibits cancer spheroid growth. PloS one. 2021;16(7):e0254315. [Content Brief]
- [3]. Beyrath J, et al. KH176 Safeguards Mitochondrial Diseased Cells from Redox Stress-Induced Cell Death by Interacting with the Thioredoxin System/Peroxiredoxin Enzyme Machinery. Scientific reports. 2018 Apr 26;8(1):6577. [Content Brief]
