| 货号 | 10009052-1mg |
| 描述 | Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.1,2,3 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. 4 AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. 5 AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. 5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. The Journal of Biological Chemisty 274, 8347-8350 (1999). 2.Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews.Cancer 2, 489-501 (2002). 3.Hennessy, B.T.,Smith, D.L.,Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews.Drug Discovery 4, 988-1004 (2005). 4.Rückle, T.,Schwarz, M.K., and Rommel, C. PI3Kγ inhibition: Towards an aspirin of the 21st century? Nature Reviews.Drug Discovery 5, 903-918 (2006). 5.Pomel, V.,Klicic, J.,Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ. Journal of Medicinal Chemistry 49, 3857-3871 (2006). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 305.3 |
| 分子式 | C14H8FNO4S |
| CAS号 | 900515-16-4 |
| 稳定性 | ≥ 1 year |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |