AS-605240 - CAS 648450-29-7
Catalog number: 648450-29-7
Category: Inhibitor
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AS605240 is a selective PI3Kgamma inhibitor, has been proved effective on several inflammatory diseases. Orally administration of AS605240 significantly prevented lung inflammation and reduced collagen deposition. AS605240 also inhibited augmented expression of TNF-alpha and IL-1beta induced by bleomycin instillation. AS605240 may be a useful in treating inflammation diseases. AS605240 may represent a promising novel agent for the future therapy of pulmonary fibrosis.
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AS 605240; AS605240; AS-605240.
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1.GRPR/PI3Kγ: Partners in Central Transmission of Itch.
Pereira PJ1, Machado GD2, Danesi GM2, Canevese FF2, Reddy VB3, Pereira TC4, Bogo MR5, Cheng YC6, Laedermann C6, Talbot S6, Lerner EA7, Campos MM8. J Neurosci. 2015 Dec 9;35(49):16272-81. doi: 10.1523/JNEUROSCI.2310-15.2015.
The gastrin-releasing peptide (GRP) and its receptor (GRPR) are important components of itch transmission. Upstream, but not downstream, aspects of GRPR signaling have been investigated extensively. We hypothesize that GRPR signals in part through the PI3Kγ/Akt pathway. We used pharmacological, electrophysiological, and behavioral approaches to further evaluate GRPR downstream signaling pathways. Our data show that GRP directly activates small-size capsaicin-sensitive DRG neurons, an effect that translates into transient calcium flux and membrane depolarization (∼ 20 mV). GRPR activation also induces Akt phosphorylation, a proxy for PI3Kγ activity, in ex vivo naive mouse spinal cords and in GRPR transiently expressing HEK293 cells. The intrathecal injection of GRP led to intense scratching, an effect largely reduced by either GRPR antagonists or PI3Kγ inhibitor. Scratching behavior was also induced by the intrathecal injection of an Akt activator.
2.The effect of pharmacological PI3Kγ inhibitor on eotaxin-induced human eosinophil functions.
Saito Y1, Takeda M2, Nishikawa J1, Konno Y1, Tamaki M1, Itoga M1, Kobayashi Y1, Moritoki Y1, Ito W1, Chihara J1, Ueki S1. Pulm Pharmacol Ther. 2014 Apr;27(2):164-9. doi: 10.1016/j.pupt.2013.11.006. Epub 2013 Dec 9.
BACKGROUND: Asthma is characterized by chronic inflammation caused by activation of immune cells including Th2 lymphocytes and eosinophils. Phosphoinositide 3-kinase (PI3K) γ deficient asthmatic mice did not develop lung eosinophilia, although the detailed mechanisms are not well known. A CC chemokine eotaxin (CCL11) plays a prominent role in developing eosinophilic inflammation through CCR3. In this study, we tested the roles of PI3Kγ in eotaxin-induced eosinophil functions using a pharmacological inhibitor.
3.Inhibition of Gαi activity by Gβγ is mediated by PI 3-kinase-γ- and cSrc-dependent tyrosine phosphorylation of Gαi and recruitment of RGS12.
Huang J1, Nalli AD, Mahavadi S, Kumar DP, Murthy KS. Am J Physiol Gastrointest Liver Physiol. 2014 May 1;306(9):G802-10. doi: 10.1152/ajpgi.00440.2013. Epub 2014 Feb 27.
Others and we have characterized several Gβγ-dependent effectors in smooth muscle, including G protein-coupled receptor kinase 2 (GRK2), PLCβ3, and phosphatidylinositol (PI) 3-kinase-γ, and have identified various signaling targets downstream of PI 3-kinase-γ, including cSrc, integrin-linked kinase, and Rac1-Cdc42/p21-activated kinase/p38 MAP kinase. This study identified a novel mechanism whereby Gβγ acting via PI 3-kinase-γ and cSrc exerts an inhibitory influence on Gαi activity. The Gi2-coupled δ-opioid receptor agonist d-penicillamine (2,5)-enkephalin (DPDPE) activated cSrc, stimulated tyrosine phosphorylation of Gαi2, and induced regulator of G protein signaling 12 (RGS12) association; all three events were blocked by PI 3-kinase (LY294002) and cSrc (PP2) inhibitors and by expression of the COOH-terminal sequence of GRK2-(495-689), a Gβγ-scavenging peptide. Inhibition of forskolin-stimulated cAMP and muscle relaxation by DPDPE was augmented by PP2, LY294002, and a selective PI 3-kinase-γ inhibitor, AS-605420.
4.The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels.
Martin KJ1, Muessel MJ1, Pullar CE2, Willars GB2, Wardlaw AJ1. PLoS One. 2015 Feb 6;10(2):e0116250. doi: 10.1371/journal.pone.0116250. eCollection 2015.
The entry of neutrophils into tissue has been well characterised; however the fate of these cells once inside the tissue microenvironment is not fully understood. A variety of signal transduction pathways including those involving class I PI3 Kinases have been suggested to be involved in neutrophil migration. This study aims to determine the involvement of PI3 Kinases in chemokinetic and chemotactic neutrophil migration in response to CXCL8 and GM-CSF in a three-dimensional collagen gel, as a model of tissue. Using a three-dimensional collagen assay chemokinetic and chemotactic migration induced by CXCL8 was inhibited with the pan PI3 Kinase inhibitor wortmannin. Analysis of the specific Class I PI3 Kinase catalytic isoforms alpha, delta and gamma using the inhibitors PIK-75, PIK-294 and AS-605240 respectively indicated differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration.
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CAS 648450-29-7 AS-605240

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