Date published: 2026-2-2

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AS-252424 (CAS 900515-16-4)

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Alternate Names:
5-(5-(4-fluoro-2-hydroxyphenyl)furan-2-ylmethylene)thiazolidine-2,4-dione
Application:
AS-252424 is a selective PI 3-kinase p110γ inhibitor
CAS Number:
900515-16-4
Purity:
>98%
Molecular Weight:
305.28
Molecular Formula:
C14H8FNO4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AS-252424 is a potent and selective PI 3-kinase p110gamma 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 muM. AS-252424 is an inhibitor of Casein Kinase and PI 3-kinase p110 alpha.


AS-252424 (CAS 900515-16-4) References

  1. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.  |  Pomel, V., et al. 2006. J Med Chem. 49: 3857-71. PMID: 16789742
  2. Insulin-like growth factor-1 regulates platelet activation through PI3-Kalpha isoform.  |  Kim, S., et al. 2007. Blood. 110: 4206-13. PMID: 17827385
  3. Overlapping and distinct roles for PI3Kbeta and gamma isoforms in S1P-induced migration of human and mouse endothelial cells.  |  Heller, R., et al. 2008. Cardiovasc Res. 80: 96-105. PMID: 18558630
  4. Phosphoinositide 3-kinase mediated signaling in lobster olfactory receptor neurons.  |  Corey, EA., et al. 2010. J Neurochem. 113: 341-50. PMID: 20132480
  5. Inhibition of PI3K prevents the proliferation and differentiation of human lung fibroblasts into myofibroblasts: the role of class I P110 isoforms.  |  Conte, E., et al. 2011. PLoS One. 6: e24663. PMID: 21984893
  6. Key role of PI3Kγ in monocyte chemotactic protein-1-mediated amplification of PDGF-induced aortic smooth muscle cell migration.  |  Fougerat, A., et al. 2012. Br J Pharmacol. 166: 1643-53. PMID: 22251152
  7. Phosphoinositide-3-kinase/akt - dependent signaling is required for maintenance of [Ca(2+)](i), I(Ca), and Ca(2+) transients in HL-1 cardiomyocytes.  |  Graves, BM., et al. 2012. J Biomed Sci. 19: 59. PMID: 22715995
  8. Phosphoinositide-3-kinases p110α and p110β mediate S phase entry in astroglial cells in the marginal zone of rat neocortex.  |  Müller, R., et al. 2013. Front Cell Neurosci. 7: 24. PMID: 23504389
  9. Phosphoinositide 3-kinase β, phosphoinositide 3-kinase δ, and phosphoinositide 3-kinase γ mediate the anti-inflammatory effects of magnesium sulfate.  |  Lee, PY., et al. 2015. J Surg Res. 197: 390-7. PMID: 25972311
  10. Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth.  |  Sweetlove, M., et al. 2015. Front Oncol. 5: 135. PMID: 26137449
  11. Potency and pharmacokinetics of broad spectrum and isoform-specific p110γ and δ inhibitors in cancers.  |  Setti, A., et al. 2016. J Recept Signal Transduct Res. 36: 26-36. PMID: 26791581
  12. Phosphoinositide 3-Kinase Is Involved in Mediating the Anti-inflammation Effects of Vasopressin.  |  Jan, WC., et al. 2017. Inflammation. 40: 435-441. PMID: 27943011
  13. The Selective Phosphoinoside-3-Kinase p110δ Inhibitor IPI-3063 Potently Suppresses B Cell Survival, Proliferation, and Differentiation.  |  Chiu, H., et al. 2017. Front Immunol. 8: 747. PMID: 28713374
  14. RXFP1 Receptor Activation by Relaxin-2 Induces Vascular Relaxation in Mice via a Gαi2-Protein/PI3Kß/γ/Nitric Oxide-Coupled Pathway.  |  Lian, X., et al. 2018. Front Physiol. 9: 1234. PMID: 30233409
  15. Phosphoproteomics Identifies PI3K Inhibitor-selective Adaptive Responses in Pancreatic Cancer Cell Therapy and Resistance.  |  Cintas, C., et al. 2021. Mol Cancer Ther. 20: 2433-2445. PMID: 34552006

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AS-252424, 1 mg

sc-202961
1 mg
$42.00

AS-252424, 5 mg

sc-202961A
5 mg
$158.00