648450-29-7 | AS-605240

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$13.00	$9.00
5mg	98%	in stock	$32.00	$22.00
10mg	98%	in stock	$53.00	$37.00
25mg	98%	in stock	$110.00	$77.00
50mg	98%	in stock	$214.00	$150.00
100mg	98%	in stock	$308.00	$216.00

Description

• Catalog Number: AD16691
• Chemical Name: AS-605240
• CAS Number: 648450-29-7
• Molecular Formula: C12H7N3O2S
• Molecular Weight: 257.2679
• MDL Number: MFCD11114066
• SMILES: O=C1NC(=O)C(=Cc2ccc3c(c2)nccn3)S1

Computed Properties

• Complexity: 410
• Covalently-Bonded Unit Count: 1
• Defined Bond Stereocenter Count: 1
• Heavy Atom Count: 18
• Hydrogen Bond Acceptor Count: 5
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 1
• XLogP3: 1.5

Literature

• A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

  The Biochemical journal 20130415

• PI3Kγ activation is required for LPS-induced reactive oxygen species generation in respiratory epithelial cells.

  Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20121101

• PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.

  Journal of medicinal chemistry 20121025

• The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes.

  Diabetes 20120601

• A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.

  Nature chemical biology 20120429

• PI3K-γ inhibition ameliorates acute lung injury through regulation of IκBα/NF-κB pathway and innate immune responses.

  Journal of clinical immunology 20120401

• PI3Kγ inhibition reduces blood pressure by a vasorelaxant Akt/L-type calcium channel mechanism.

  Cardiovascular research 20120101

• Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL.

  Journal of lipid research 20120101

• Inhibition of phosphatidylinositol-3 kinase γ reduces pruriceptive, inflammatory, and nociceptive responses induced by trypsin in mice.

  Pain 20111201

• Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

  Nature biotechnology 20111101

• PI3Kγ is required for NMDA receptor-dependent long-term depression and behavioral flexibility.

  Nature neuroscience 20111023

• A novel binding assay identifies high affinity ligands to the rosiglitazone binding site of mitoNEET.

  Bioorganic & medicinal chemistry letters 20110915

• Semaphorin-PlexinD1 signaling limits angiogenic potential via the VEGF decoy receptor sFlt1.

  Developmental cell 20110816

• Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.

  Bioorganic & medicinal chemistry letters 20110815

• [The antagonistic effect of PI3K-gamma inhibitor AS605240 on cardiac hypertrophy and cardiac fibrosis induced by isoproterenol in rats].

  Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition 20110701

• Acylated and unacylated ghrelin attenuate isoproterenol-induced lipolysis in isolated rat visceral adipocytes through activation of phosphoinositide 3-kinase γ and phosphodiesterase 3B.

  Biochimica et biophysica acta 20110601

• Inhibitor of PI3Kγ ameliorates TNBS-induced colitis in mice by affecting the functional activity of CD4+CD25+FoxP3+ regulatory T cells.

  British journal of pharmacology 20110501

• Integrating cardiac PIP3 and cAMP signaling through a PKA anchoring function of p110γ.

  Molecular cell 20110408

• Remodeling of VE-cadherin junctions by the human herpes virus 8 G-protein coupled receptor.

  Oncogene 20110113

• Targeting PI3K in neuroblastoma.

  Journal of cancer research and clinical oncology 20101201

• Fibroblast growth factor 2 and platelet-derived growth factor, but not platelet lysate, induce proliferation-dependent, functional class II major histocompatibility complex antigen in human mesenchymal stem cells.

  Arthritis and rheumatism 20101201

• Pharmacologic inhibition of phosphoinositide 3-kinase gamma (PI3Kγ) promotes infarct resorption and prevents adverse cardiac remodeling after myocardial infarction in mice.

  Journal of cardiovascular pharmacology 20101201

• Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.

  Bioorganic & medicinal chemistry letters 20100901

• Effects of PI3Kgamma inhibition using AS-605240 in acute myocardial infarction.

  Circulation research 20100723

• A phosphoinositide 3-kinase-gamma inhibitor, AS605240 prevents bleomycin-induced pulmonary fibrosis in rats.

  Biochemical and biophysical research communications 20100625

• Phosphoinositide 3-kinase gamma required for lipopolysaccharide-induced transepithelial neutrophil trafficking in the lung.

  The European respiratory journal 20100501

• Involvement of phosphoinositide 3-kinase gamma in angiogenesis and healing of experimental myocardial infarction in mice.

  Circulation research 20100305

• Discovery of (Z)-5-(4-methoxybenzylidene)thiazolidine-2,4-dione, a readily available and orally active glitazone for the treatment of concanavalin A-induced acute liver injury of BALB/c mice.

  Journal of medicinal chemistry 20100114

• Inhibition of phosphoinositide 3-kinase ameliorates dextran sodium sulfate-induced colitis in mice.

  The Journal of pharmacology and experimental therapeutics 20100101

• Phosphoinositol 3-kinase-gamma mediates antineutrophil cytoplasmic autoantibody-induced glomerulonephritis.

  Kidney international 20100101

• Phosphoinositide 3-kinase gamma inhibitor ameliorates concanavalin A-induced hepatic injury in mice.

  Biochemical and biophysical research communications 20090904

• Insulin granule recruitment and exocytosis is dependent on p110gamma in insulinoma and human beta-cells.

  Diabetes 20090901

• [Intervention effect of PI3Kgamma inhibitor AS605240 on autoimmune myocarditis in mice].

  Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition 20090901

• PI3Kgamma differentially regulates FcepsilonRI-mediated degranulation and migration of mast cells by and toward antigen.

  International archives of allergy and immunology 20090101

• Genetic and pharmacological targeting of phosphoinositide 3-kinase-gamma reduces atherosclerosis and favors plaque stability by modulating inflammatory processes.

  Circulation 20080311

• [Therapeutic potential of phosphoinositide 3-kinase inhibitors in rheumatoid arthritis].

  Nihon Rinsho Men'eki Gakkai kaishi = Japanese journal of clinical immunology 20071001

• Importance of phosphoinositide 3-kinase gamma in the host defense against pneumococcal infection.

  American journal of respiratory and critical care medicine 20070501

• Phosphoinositide 3-kinase-gamma as a target in rheumatoid arthritis and systemic lupus.

  Expert opinion on therapeutic targets 20060801

• PI3Kgamma inhibition blocks glomerulonephritis and extends lifespan in a mouse model of systemic lupus.

  Nature medicine 20050901

• Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

  Nature medicine 20050901

• Modulating autoimmunity: pick your PI3 kinase.

  Nature medicine 20050901

• Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.

  The Journal of biological chemistry 20020419