| Bioactivity | PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation[1]. |
| Invitro | PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC50 value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a 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 an IC50 value of 4.1 μM[1]. |
| In Vivo | 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.; injected at 4 hours and 24 hours after ischemia onset) reduces the infarct volume and improves neurological deficits of tMCAO rats[1]. Animal Model: |
| Name | PKM2-IN-3 |
| CAS | 2408841-19-8 |
| Formula | C21H22O4 |
| Molar Mass | 338.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |