AS-252424
Catalog No.S2671
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.
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
Choose Selective PI3K Inhibitors
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 |
|
|||||||||||||||||||||||
| 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 |
|
|||||||||||||||||||||||
| 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
|
| Animal Research:[1] |
+ Expand
|
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 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
