AS-604850 |
カタログ番号GC12080 |
AS-604850 は、0.25 μM の IC50 値と 0.18 μM の Ki 値を持つ強力で選択的な ATP 競合 PI3Kγ 阻害剤です。 AS-604850 は、PI3Kδ および β に対して 30 倍以上の選択性、PI3Kα に対してそれぞれ 18 倍の選択性を持つ PI3Kγ のアイソフォーム選択的阻害剤を示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 648449-76-7
Sample solution is provided at 25 µL, 10mM.
AS-604850 is a selective and ATP-competitive PI3Kγ inhibitor (IC50= 2.5 μM), with over 30-fold selectivity for PI3Kδ and PI3Kβ, and 18-fold selectivity over PI3Kα. [1]
PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt(PKB)/mTOR pathway.
In rat hepatocytes, AS-604850 pretreatment abolished GCDC-induced phosphorylation of Akt by 50% and inhibited apoptosis by reducing GCDC/TCDC/TLC-induced caspase-3 cleavage. [2] In PI3KCG-/-monocytes and THP-1 (human monocytic cell line), AS-604850 inhibited the PKB phosphorylation activated by MCP-1, it also blocked the MCP-1-mediated chemotaxis in a concentration dependent manner. In RAW264 mouse macrophages, C5a-mediated PKB phosphorylation was inhibited by AS-604850. [1]
In the thioglycollate-induced peritonitis model that induced multiple chemokine in vivo, oral administration of 10 mg/kg AS-604850 showed a 31% decrease of neutrophil recruitment. [1]
References:
1. Camps M, Rückle T, Ji H et al. Blockade of PI3K-gamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43.
2. Hohenester S, Gates A, Wimmer R et al. Phosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells. J Hepatol. 2010 Nov;53(5):918-26.
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