PKM2-IN-3

PKM2-IN-3 is a inhibitor of PKM2 kinase with IC50 value of 4.1μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation[1].

Research Areas >> Neurological Disease

4.1 μM (PKM2)

PKM2-IN-3 inhibit the TNF-α release of LPS-stimulated RAW264.7 macrophages, with IC50 value of 5.2 μM. PKM2-IN-3 exhibited the lowest toxicity with CC50 value of 43.6 μM[1]. PKM2-IN-3 (0.1-100 μM; 20 min) inhibits PKM2 kinase activity in a cell-free molecular level with the IC50 value of 4.1 μm[1].

PKM2-IN-3 (1, 10 mg/kg; i.p.; daily for 3 days ) significantly reverses the LPS-induced mice behavior changes in open field test[1]. PKM2-IN-3 (1, 10 mg/kg, i.v.; inject at 4 hours and 24 hours after ischemia onset) reduces the infarct volume and improves neurological deficits of tMCAO rats[1]. Animal Model: LPS-induced mice (male 6-8 weeks old; 20.0-22.0 g)[1] Dosage: 1, 10 mg/kg Administration: i.p.; daily for 3 days Result: Reversed the LPS-induced mice behavior changes in open field test. Animal Model: tMCAO Sprague-Dawley rats (Male 8-10 weeks old; 250.0-280.0 g)[1] Dosage: 1, 10 mg/kg Administration: i.v.; injected at 4 hours and 24 hours after ischemia onset Result: Reduced the infarct volume and improved neurological deficits of tMCAO rats.

[1]. Gao CL, et al. Synthesis and Target Identification of Benzoxepane Derivatives as Potential Anti-Neuroinflammatory Agents for Ischemic Stroke. Angew Chem Int Ed Engl. 2020;59(6):2429-2439.