Home PI3K/Akt/mTOR PI3K inhibitor AS-252424 For research use only.

AS-252424

AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.

AS-252424 Chemical Structure

AS-252424 Chemical Structure

CAS No. 900515-16-4

Purity & Quality Control

AS-252424 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse Raw264 macrophage Function assay Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=0.23 μM 16789742
THP1 cells Function assay Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=0.4 μM 16789742
Click to View More Cell Line Experimental Data

Biological Activity

Description AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
Targets
Casein Kinase 2 [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)		 PI3Kα [1]
(Cell-free assay)
20 nM 33 nM 935 nM
In vitro
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. [1] AS252424 specifically blocks proliferation in the pancreatic cancer cell lines HPAF and Capan1, as assessed by cell counting. [2] A recent research indicates 100 nM of AS-252424 significantly reduces [Ca2+]i, ICa and Ca2+ transients in HL-1 cardiomyocytes. [3]
Kinase Assay In vitro PI3Kγ Kinase Assay
Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi γ[33]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of AS-252424 or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded.
Cell Research Cell lines Raw-264 macrophage
Concentrations 0.01 nM to 0.1 μM
Incubation Time 5 minutes
Method 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.
In Vivo
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. [1]
Animal Research Animal Models Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
Dosages 10 mg/kg
Administration Oral administration 15 minutes before injection of thioglycollate

Chemical Information & Solubility

Molecular Weight 305.28 Formula

C14H8FNO4S
CAS No. 900515-16-4 SDF Download AS-252424 SDF
Smiles C1=CC(=C(C=C1F)O)C2=CC=C(O2)C=C3C(=O)NC(=O)S3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (199.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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