AS-252424

SKU: orb1300979

Description

AS-252424

Research Area

Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 900515-16-4
• MW: 305.28
• Purity: 99.26%
• Formula: C₁₄H₈FNO₄S
• SMILES: Oc1cc(F)ccc1-c1ccc(\C=C2/SC(=O)NC2=O)o1
• Target: PI3K,Casein Kinase
• Solubility: DMSO:47.5 mg/mL (155.59 mM)

Bioactivity

• Target IC50:
  PI3Kα:935 nM|PI3Kβ:20 μM|PI3Kγ:33 nM|PI3Kδ:20 μM
• In Vivo:
  Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%), almost matching the result observed in PI3Kγ-deficient mice.
• In Vitro:
  AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. AS-252424 shows reduced potency on PI3Kα with an IC50 with 935 nM. When screening against 80 different Ser/Thr and Tyr kinases, AS-252424 doesn't show significant inhibit towards any of them at 10 μM except for CK2. AS-252424 inhibits C5a-mediated PKB/Akt phosphorylation in a concentration- dependent manner with submicromolar or low-micromolar IC50 value. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. A recent research indicates 100 nM of AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes.
• Cell Research:
  After 3 hours of starvation in serum-free medium, Raw-264 macrophages are pretreated with AS-252424 or DMSO for 30 minutes and stimulated for 5 minutes with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PI3Kγ, PI3Kα, PI3K, Phosphoinositide 3-kinase, inhibit, Inhibitor, Casein Kinase, CaseinKinase, AS252424, AS-252424, AS 252424, CK2

Compound Identifiers

PubChem CID

11630874