Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC 50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect.
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5 mg | Inquiry | $ 970.00 |
Description | PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC 50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect. |
Targets&IC50 | PKM2:4.1 μM (IC50) |
In vitro | PKM2-IN-3 (compound 10i) effectively suppresses TNF-α secretion in LPS-induced RAW264.7 macrophages at an IC50 of 5.2 μM and demonstrates minimal toxicity, evidenced by a CC50 of 43.6 μM[1]. Additionally, at concentrations ranging from 0.1 to 100 μM over a 20-minute period, PKM2-IN-3 selectively inhibits PKM2 kinase activity at a molecular level, achieving an IC50 of 4.1 μM[1]. |
In vivo | PKM2-IN-3, at a dosage of 1 and 10 mg/kg administered intraperitoneally (i.p.) daily for three days, significantly reversed behavior changes in LPS-induced mice during open field tests. Similarly, when administered intravenously (i.v.) at 4 hours and 24 hours post-ischemia, it notably reduced infarct volume and ameliorated neurological deficits in tMCAO rat models. In the first scenario, the treatment involved male mice aged 6-8 weeks and weighing 20.0-22.0 g, while in the second, male Sprague-Dawley rats aged 8-10 weeks and weighing 250.0-280.0 g were used. |
Synonyms | PKM2-IN-3 |
Molecular Weight | 338.403 |
Formula | C21H22O4 |
CAS No. | 2408841-19-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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PKM2-IN-3 2408841-19-8 PKM2 IN 3 PKM2IN3 PKM-2-IN-3 inhibitor inhibit