PI-828

CAS号

942289-87-4

分子式

C19H18N2O3

主要靶点

Casein Kinase|PI3K

仅限科研使用

Cat No : CM10733

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Synonyms

Casein Kinase|CaseinKinase|CK2α2|CK2|p110α|PI828|PI-828|PI 828|LY 294002, 4gamma-NH2|LY294002|LY-294002, 4gamma-NH2



产品信息

CAS号 942289-87-4
分子式 C19H18N2O3
主要靶点 Casein Kinase|PI3K
主要通路 PI3K/Akt/mTOR 信号通路|干细胞|代谢
分子量 322.36
纯度 99.39%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Casein Kinase|CaseinKinase|CK2α2|CK2|p110α|PI828|PI-828|PI 828|LY 294002, 4gamma-NH2|LY294002|LY-294002, 4gamma-NH2

靶点活性

CK2α2:1.127 μM|p110α:173 nM|CK2:149 nM

体外活性

PI-828(0.78-3.12 μM;48小时)降低半胱天冬酶3激活。然而,较高浓度的PI-828(6.25-12.5 μM)单独使用可引起凋亡[2]。PI-828对PI3K-C2β的敏感性是其关键特征,表现出与I类PI3K不同的敏感性。值得注意的是,1 μM的PI-828对PI3K-C2β的活性无影响,而显著抑制I类PI3K。特别是,10 μM的PI-828完全阻断I类PI3K,而对PI3K-C2β只有部分抑制效果[4]。

溶解度

DMSO:11.2 mg/mL (34.74 mM)

参考文献

1.Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.
2.Kulkarni AA, et al. Supramolecular nanoparticles that target phosphoinositide-3-kinase overcome insulin resistance and exert pronounced antitumor efficacy. Cancer Res. 2013 Dec 1;73(23):6987-97.
3.McLean AB, et al. Activin a efficiently specifies definitive endoderm from human embryonic stem cells only when phosphatidylinositol 3-kinase signaling is suppressed. Stem Cells. 2007 Jan;25(1):29-38.
4.Falasca M, Maffucci T. Emerging roles of phosphatidylinositol 3-monophosphate as a dynamic lipid second messenger. Arch Physiol Biochem. 2006 Oct-Dec;112(4-5):274-84.

The molarity calculator equation

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The dilution calculator equation

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