Ogasawara, Daisuke’s team published research in Journal of Medicinal Chemistry in 2019-02-14 | CAS: 132097-09-7

Journal of Medicinal Chemistry published new progress about Crystal structure. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Product Details of C6H5Cl2N.

Ogasawara, Daisuke published the artcileDiscovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12), Product Details of C6H5Cl2N, the main research area is lysophosphatidylserine lipase hydrolase domain 12 ABHD12 inhibitor.

ABHD12 is a membrane-bound hydrolytic enzyme that acts on the lysophosphatidylserine (lyso-PS) and lysophosphatidylinositol (lyso-PI) classes of immunomodulatory lipids. Human and mouse genetic studies point to a key role for the ABHD12-(lyso)-PS/PI pathway in regulating (neuro)immunol. functions in both the central nervous system and periphery. Selective inhibitors of ABHD12 would offer valuable pharmacol. probes to complement genetic models of ABHD12-regulated (lyso)-PS/PI metabolism and signaling. Here, we provide a detailed description of the discovery and activity-based protein profiling (ABPP) guided optimization of reversible thiourea inhibitors of ABHD12 that culminated in the identification of DO264 as a potent, selective, and in vivo active ABHD12 inhibitor. We also show that DO264, but not a structurally related inactive control probe (S)-DO271, augments inflammatory cytokine production from human THP-1 macrophage cells. The in vitro and in vivo properties of DO264 designate this compound as a suitable chem. probe for studying the biol. functions of ABHD12-(lyso)-PS/PI pathways.

Journal of Medicinal Chemistry published new progress about Crystal structure. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Product Details of C6H5Cl2N.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem