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AS-252424

Chemical Structure : AS-252424

CAS No.: 900515-16-4

AS-252424 (AS252424)

Catalog No.: PC-22458Not For Human Use, Lab Use Only.

AS-252424 is a potent, and selective inhibitor of phosphoinositide 3-kinase gamma (PI3Kγ) with IC50 of 30 nM, 30-fold selective over PI3Kα, also is a potent ferroptosis inhibitor targeting ACSL4.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AS-252424 is a potent, and selective inhibitor of phosphoinositide 3-kinase gamma (PI3Kγ) with IC50 of 30 nM, 30-fold selective over PI3Kα, also is a potent ferroptosis inhibitor targeting ACSL4.
AS-252424 displays no significant activity over PI3Kβ/δ (IC50>20 uM), as well as excellent selectivity profile against a large set of unrelated protein kinases.
AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration-dependent manner in Raw-264 macrophages (IC50=0.228 uM), with no effect on SCF-induced phosphorylation of PKB/Akt in bone marrow derived mast cells.
AS-252424 inhibits preferentially chemokine-induced (PI3Kγ-mediated) but not cytokine-induced (class IA PI3K-mediated) PKB/Akt phosphorylation in the human monocytic cell line THP-1.
AS-252424 decreases leukocyte infiltration in a murine peritonitis model.
AS-252424 also is a potent ferroptosis inhibitor, directly binds to the glutamine 464 of ACSL4 to inhibit its enzymatic activity.

Physicochemical Properties

M.Wt 305.28
Formula C14H8FNO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-5-((5-(4-Fluoro-2-hydroxyphenyl)furan-2-yl)methylene)thiazolidine-2,4-dione

References

1. Pomel V, et al. J Med Chem. 2006 Jun 29;49(13):3857-71.

2. Huang Q, et al. Sci Adv. 2024 Mar 29;10(13):eadk1200.

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