AS 605240

Cat. No. 3578

AS 605240 C12H7N3O2S [648450-29-7]

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Chemical Name: 5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione

Biological Activity

Potent and selective inhibitor of PI 3-kinase γ (PI 3-Kγ) (IC50 = 8 nM). Displays 30-fold selectivity over PI 3-Kδ and PI 3-Kβ and 7.5-fold selectivity over PI 3-Kα. Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis. Orally active and ATP-competitive.

Technical Data

M.Wt:
257.27
Formula:
C12H7N3O2S
Solubility:
Soluble to 1 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
648450-29-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Peng et al (2010) Inhibition of phosphoinositide 3-kinase ameliorates dextran sodium sulfate-induced colitis in mice. J.Pharmacol.Exp.Ther. 332 46. PMID: 19828878.

Wang et al (2009) Phosphoinositide 3-kinase γ inhibitor ameliorates concanavalin A-induced hepatic injury in mice. Biochem.Biophys.Res.Comm. 386 569.

Camps et al (2005) Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nature Med. 11 936.

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Citations are publications that use Tocris products. Selected citations for AS 605240 include:

Beauséjour et al (2012) Integrin/Fak/Src-mediated regulation of cell survival and anoikis in human intestinal epithelial crypt cells: selective engagement and roles of PI3-K isoform complexes. Apoptosis 17 566. PMID: 22402981.

Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832. PMID: 22434859.

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View Related Products by Product Action

Keywords: AS 605240, supplier, AS605240, PI3Kgamma, PI3Kγ, PI, 3-kinasegamma, 3-kinaseg, 3-kinaseγ, phosphoinositide, 3, kinases, gamma, γ, Potent, selective, inhibitors, inhibits, inositol, lipids, signalling, signaling, orally, active, ATP-competitive, Tocris Bioscience, PI 3-kinase Inhibitor products

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