| Name | AS-252424 |
| Description | AS-252424 is a potent and selective inhibitor of PI3Kγ with an IC50 of 33 nM and demonstrates over 10-fold selectivity for PI3Kγ versus PI3Kα. |
| 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) |
| 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. |
| 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] |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (147.41 mM)
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| Keywords | inhibit | Phosphoinositide 3-kinase | PI3K | Inhibitor | AS 252424 | AS-252424 | AS252424 |
| Inhibitors Related | Myricetin | Erucic acid | Sapanisertib | Emodin | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Prostate Cancer Compound Library | Immuno-Oncology Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Neuronal Differentiation Compound Library |
United States
