mbm 17s

MBM-17S, a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM, effectively inhibits cancer cell proliferation by inducing cell cycle arrest and apoptosis. It demonstrates antitumor activities without evident toxicity to mice.

6-[(3S,8S,9S,10R,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxo-1H-pyridine-3,4-dicarbonitrile 是一种生物活性化合物，可用于化学和生命科学领域的研究。

Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to be determined. 1.Serhan, C.N., Gotlinger, K., Hong, S., et al.Anti-inflammatory actions of neuroprotectin D1/protectin D1 and its natural stereoisomers: Assignments of dihydroxy-containing docosatrienesJ. Immunol.176(3)1848-1859(2006) 2.Ariel, A., and Serhan, C.N.Resolvins and protectins in the termination program of acute inflammationTRENDS in Immunology28(4)176-183(2007) 3.Schwab, J.M., Chiang, N., Arita, M., et al.Resolvin E1 and protectin D1 activate inflammation-resolution programmesNature447(7146)869-874(2007)

Protectin D1 (also known as neuroprotectin D1 when produced in neuronal tissues) is a DHA-derived dihydroxy fatty acid that exhibits potent protective and anti-inflammatory activities. 10(S),17(S)-DiHDHA is a DHA metabolite, also referred to as protectin DX (PDX). It is produced by an apparent double lipoxygenase (LO)-mediated reaction in murine peritonitis exudates, in suspensions of human leukocytes, or by soybean 15-LO incubated with DHA. It differs from protectin D1 with respect to the stereochemistry of the C-10 hydroxyl and the double bond configuration at the 13 and 15 positions. 10(S),17(S)-DiHDHA blocks neutrophil infiltration in murine peritonitis by 20-25% at a dose of 1 ng/mouse. It also inhibits platelet activation by both impairing thromboxane (TX) synthesis and TX receptor activation.

17(S)-HpDHA为主要由15-Lipoxygenase（LOX）同工酶：h15-LOX-1和h15-LOX-2与二十二碳六烯酸(DHA)反应生成。该化合物通过变构负向调控环氧化物合成，且能够抑制血小板聚集，其EC50值约为1μM。

17(S)-HDoTE, a metabolite of adrenic acid, is synthesized through the action of 15-lipoxygenase (15-LO) via a 17-HpDoTE intermediate.

17(S)-HDHA is a primary mono-oxygenation product of docosahexaenoic acid in human whole blood, human leukocytes, and mouse brain. 17(S)-HDHA serves as a precursor to 17(S)-resolvins and has intrinsic biological activity, such as the inhibition of TNF-α-induced interleukin-1β expression in human glioma cells and inhibition of TNF-α-induced leukocyte trafficking to the mouse air pouch.

MBM-17 is a potent inhibitor of NIMA-related kinase 2 (Nek2,IC50 of 3 nM). It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites.17-HETE is a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney.17(S)-HETE inhibits proximal tubule ATPase activity by as much as 70% at a concentration of 2 μM.

17(R,S)-Benzo-resolvin D1 (benzo-RvD1) 是专门的分辨介质 (SPM) RvD1 的衍生物。在10和100 nM的浓度下，它能减少PDGF-BB诱导的人类血管平滑肌细胞 (VSMCs) 的细胞骨架变化，并抑制PDGF诱导的这些细胞的迁移。Benzo-RvD1 (10 nM) 抑制人脐静脉内皮细胞 (HUVECs) 中的p65核转位。它还提高了RAW 264.7对S. aureus和zymosan颗粒的吞噬作用。