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- PKD (Protein kinase D)
- AS-605240 (potassium salt)
AS-605240 (potassium salt)
A potent inhibitor of PI3Kγ
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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1mg￥512.00410.00- +
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5mg￥2337.001870.00- +
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10mg￥4100.003280.00- +
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25mg￥9000.007200.00- +
- 货号: ajcx18116
- CAS: N/A
- 别名:
- 分子式: C12H6N3O2S?K
- 分子量: 295.4
- 纯度: ＞98%
- 溶解度: DMF: 3 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
- 储存: Store at -20°C
- 库存: 现货
Background
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis. It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively. AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg. AS-605240 (potassium salt) has improved solubility compared to AS-605240 .
