A potent inhibitor of PI3K with selectivity for the g isoform; inhibits human recombinant PI3Kg

AS-252424 – 1 mg

Brand:
Cayman
CAS:
900515-16-4
Storage:
-20
UN-No:
Non-Hazardous - /

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}  

 

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SKU: 10009052 - 1 mg Category:

Description

A potent inhibitor of PI3K with selectivity for the g isoform; inhibits human recombinant PI3Kg, a, d, with IC50 values of 30, 940, 20,000, and 20,000 nM, respectively

Formal name: 5-[5-(4-fluoro-2-hydroxy-phenyl)-furan-2-ylmethylene]-thiazolidine-2,4-dione

Synonyms: 

Molecular weight: 305.3

CAS: 900515-16-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Immunology & Inflammation|Innate Immunity

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