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AS-252424

Catalog No. T6208 CAS 900515-16-4

AS-252424 is a potent and selective inhibitor of PI3Kγ with IC50 of 33 nM; <10 fold selectivity for PI3Kγ versus PI3Kα.

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AS-252424, CAS 900515-16-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 46.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 137.00
25 mg	In stock	$ 228.00
50 mg	In stock	$ 343.00
100 mg	In stock	$ 497.00
500 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99.26%

Purity: 99.06%

Biological Description

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Description	AS-252424 is a potent and selective inhibitor of PI3Kγ with IC50 of 33 nM; >10 fold selectivity for PI3Kγ versus PI3Kα.
Targets&IC50	PI3Kγ:33 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]
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]
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	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)

Molecular Weight	305.28
Formula	C14H8FNO4S
CAS No.	900515-16-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30.5 mg/mL (100 mM)

References and Literature

1. Pomel V, et al, J Med Chem, 2006, 49(13), 3857-3871. 2. Edling CE, et al, Clin Cancer Res, 2010, 16(20), 4928-4937. 3. Graves BM, et al, J Biomed Sci, 2012, 19(1), 59 [Epub ahead of print]

Citations

1. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Glycolysis Compound Library Anti-Pancreatic Cancer Compound Library Anti-Aging Compound Library Oxidation-Reduction Compound Library Neural Regeneration Compound Library Anti-Obesity Compound Library Anti-Cancer Metabolism Compound Library Bioactive Lipid Compound Library

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Keywords

AS-252424 900515-16-4 Metabolism PI3K/Akt/mTOR signaling Stem Cells PI3K Casein Kinase inhibit Phosphoinositide 3-kinase Inhibitor AS 252424 AS252424 inhibitor

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