AS-252424

Catalog No.S2671

AS-252424 Chemical Structure

Molecular Weight(MW): 305.28

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.

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3 Customer Reviews

  • The concentrations of a tumor necrosis factor-α (TNF-α), b interleukin-6 (IL-6), and c macrophage inflammatory protein-2 (MIP-2) in lipopolysaccharide (LPS)-activated RAW264.7 cells measured by enzyme-linked immunosorbent assay. LPS: the LPS (100 ng/mL) group. LPS+V: the LPS plus vasopressin (100 pg/mL) group. LPS+V+LY: the LPS plus vasopressin plus nonspecific PI3K inhibitor LY294002 (10 μM) group. LPS+V+PIK: the LPS plus vasopressin plus specific PI3Kα inhibitor PIK-75 (50 nM) group. LPS+V+TGX: the LPS plus vasopressin plus specific PI3Kβ inhibitor TGX-221 (50 nM) group. LPS+V+IC: the LPS plus vasopressin plus specific PI3Kδ inhibitor IC-87114 (5 μM) group. LPS+V+AS: the LPS plus vasopressin plus specific PI3Kγ inhibitor AS-252424 (300 nM) group. Data were derived from six culture dishes from each group and expressed as the means ± standard errors. *P < 0.05, the LPS+V group versus the LPS group; #P < 0.05, versus the LPS+V group.

    Inflammation, 2017, 40(2):435-441. AS-252424 purchased from Selleck.

    Effects of AS252424 on KL-induced cPLA 2 phosphorylation in BMMCs. BMMCs were pre-incubated with AS252424 for 1 h followed by stimulation with KL for 15 min. The phosphorylation of cPLA 2 was evaluated via immunoblot analysis. Results are representative of three independent experiments.*P<0.05, **P<0.01, ***P<0.001 and ### P<0.001, compared with BMMCs with KL induction but without pretreatment by AS252424.

    Inflammation 2014 37(4), 1254-60. AS-252424 purchased from Selleck.

  • After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of AS-252424 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. AS-252424 purchased from Selleck.

Purity & Quality Control

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse Raw264 macrophage M3nucmZ2dmO2aX;uJIF{e2G7 NIP6d|NKdmirYnn0bY9vKG:oIFO1ZU1u\WSrYYTl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDSZZczPjRibXHjdo9xcGGpZTygTWM2OD1yLkKzJO69VQ>? MUmxOlc5QTd2Mh?=
THP1 cells MnPNSpVv[3Srb36gZZN{[Xl? M1iz[GlvcGmkaYTpc44hd2ZiTVPQNU1qdmS3Y3XkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJHRJWDFiY3XscJMtKEmFNUC9NE41KM7:TR?= Ml35NVY4QDl5NEK=

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
+ Expand

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:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Intraperitoneally injecting female C3H mice with thioglycollate (40 ml/kg) to induced a peritonitis mouse model
  • Formulation: AS-252424 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
  • Dosages: 10 mg/kg
  • Administration: Oral administration 15 minutes before injection of thioglycollate
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (199.81 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
4% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 305.28
Formula

C14H8FNO4S

CAS No. 900515-16-4
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID