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.
Cited by 8 Publications
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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.
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|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.|
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. 
|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 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 γATP, 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.
|In vitro||DMSO||61 mg/mL (199.81 mM)|
|In vivo||Add solvents individually and in order:
4% DMSO+50% PEG 300+5% Tween 80+ddH2O
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