AS-252424 is a potent and selective PI 3-kinase p110γ inhibitor (IC50 = 33 nM) shown to be selective for class IB PI 3-kinase-mediated cellular effects. AS-252424 also prevents C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 of 0.23 μM. AS-252424 is an inhibitor of Casein Kinase and PI 3-kinase p110 α.
Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils: A.M. Condliffe, et al.; Blood 106, 1432 (2005) Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma: V. Pomel, et al.; J. Med. Chem. 49, 3857 (2006)
Soluble in DMSO (~20 mg/ml), 100% ethanol (10 mg/ml), DMF (~20 mg/ml), and 1:1 solution of DMSO:PBS, pH 7.4 (0.5 mg/ml).
Store at -20° C
256.33° C (Predicted)
593.61° C (Predicted)
~1.6 g/cm3 (Predicted)
n20D 1.69 (Predicted)
PI 3-Kγ : IC50 = 30 nM; C5a-mediated phosphorylation of Akt: IC50 = 0.23 µM (RAW 264.7 macrophages ); PI 3-Kα : IC50 = 0.94 µM; MKK7β: IC50 = >10 µM; PI 3-Kβ: IC50 = 20 µM; PI 3-Kδ: IC50 = 20 µM
pKa: 7.21 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Rated 5 out of
Jin et alJin et al. (PubMed ID 24577728) found that AS-252424 reduced inflammatory responses in mouse bone marrow-derived mast cells by attenuating LTC4 production, decreasing phospholipase A2 phosphorylation and inhibiting MAPK-regulated calcium secretion. -SCBT Publication Review
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