Casein Kinase inhibitor A86 T39482

Product Introduction
Bioactivity


英文名: Casein Kinase inhibitor A86

描述: Casein Kinase inhibitor A86 is a highly effective and orally bioavailable inhibitor of casein kinase 1α (CK1α). Additionally, it displays inhibitory actions towards CDK7 (TFIIH) and CDK9 (P-TEFb). Furthermore, Casein Kinase inhibitor A86 demonstrates the ability to induce apoptosis in leukemia cells, portraying substantial anti-leukemic effects.

体外活性: 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[1]. 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)[1]. Cell Viability Assay[1]Cell 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.

体内活性: 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)[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Casein Kinase inhibitor A-86

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途