Cat. No. 3578
Chemical Name: 5-(6-Quinoxalinylmethylene)-2,4-thi
Biological ActivityPotent 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.
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 / 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.
If you know of a relevant reference for this product please let us know.
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.
Do you know of a great paper that uses AS 605240 from Tocris? If so please let us know.
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, inositol, lipids, signalling, signaling, orally, active, ATP-competitive, Tocris Bioscience, PI 3-kinase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Selective ATP competitive SphK1 and 2 inhibitor; cell permeableAkti-1/2
Potent and selective dual Akt1 and 2 inhibitorVX 680
High affinity and selective Aurora kinase inhibitorImatinib mesylate
Potent and selective v-Abl tyrosine kinase inhibitor; also inhibits PDGFR and c-kitTGX 221
Potent and selective PI 3-kinase β inhibitorPF 543 hydrochloride
Potent and selective SphK1 inhibitorJX 06
Potent and selective PDK1/2/3 inhibitorMRT 68601 hydrochloride
Potent TBK1 inhibitorAzoramide
Unfolded protein response (UPR) modulatorLCB 03-0110 dihydrochloride
Potent c-SRC kinase inhibitor; also inhibits DDR2, BTK and SykCCT 241533 dihydrochloride
Potent Chk2 inhibitorIRAK1/4 Inhibitor I
IRAK4 and IRAK1 inhibitorCentrinone
High affinity and selective PLK4 inhibitorAZD 3147
Potent and selective dual mTORC1 and 2 inhibitor; orally bioavailableTilfrinib
Potent and selective breast tumor kinase (Brk) inhibitor
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.