1. Metabolic Enzyme/Protease
  2. Pyruvate Kinase
  3. PKM2-IN-3

PKM2-IN-3 

Cat. No.: HY-139667
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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.

For research use only. We do not sell to patients.

PKM2-IN-3 Chemical Structure

PKM2-IN-3 Chemical Structure

CAS No. : 2408841-19-8

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Description

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].

IC50 & Target[1]

PKM2

4.1 μM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

338.40

Formula

C₂₁H₂₂O₄

CAS No.
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PKM2-IN-3
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