Casein Kinase inhibitor A86
规格
| Cas Number | 2079069-01-3 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 12.5 mg/mL (36.29 mM; ultrasonic and warming and heat to 60°C) |
| 过滤标签 | CDK,Casein Kinase,Cell Cycle/DNA Damage,Stem Cell/Wnt |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | 酪蛋白激酶抑制剂 A86 是一种强效口服活性酪蛋白激酶 1α (CK1α) 抑制剂。酪蛋白激酶抑制剂 A86 还能抑制 CDK7（TFIIH）和 CDK9（P-TEFb）。酪蛋白激酶抑制剂 A861 可诱导白血病细胞凋亡，并具有强效的抗白血病作用。 |
| 英文描述 |
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb) . Casein Kinase inhibitor A861 induces leukemia cell apoptosis , and has potent anti-leukemic activities In Vitro Casein Kinase inhibitor A86 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53. Casein Kinase inhibitor A86 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A86 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MV4-11 cells Concentration: 0.08 μM, 0.6 μM, 2 μM Incubation Time: 6.5 hours Result: Abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. In Vivo Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a T max of 0.2-0.5 hr, C max of 1115 ng/mL, T 1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CKIα CDK7 0.31 nM (Kd) CDK9 5.4 nM (Kd) |