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概述
Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis , and has potent anti-leukemic activities
In Vitro
Similar to CKIα depletion, Casein Kinase inhibitor A51 (0.05-3.2 μM; 18 hours) treatment of RKO cells abolished most of the Ser45 phosphorylation signal and the consecutive GSK3 phosphorylation cascade resulting in stabilization of β-catenin. Casein Kinase inhibitor A51 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 A51 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A51 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
Oral treatment is initiated at 8 days (Casein Kinase inhibitor A51; 5 mg/kg/day) after leukemia cell inoculation, at which the percentage of leukemia cells in the BM is more than 1.5% of all cells. all A51-treated mice have normal organ morphology and histology and normal blood counts . Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A51 at 20 mg/kg reveal rapid oral absorption with a T max of 0.5-2 hr, C max of 1060 ng/mL, T 1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:CKIα CDK7 1.3 nM (Kd) CDK9 4 nM (Kd)
规格
别名
酪蛋白激酶抑制剂 A51
规格或纯度
10mM in DMSO
英文名称
Casein Kinase inhibitor A51
生化机理
酪蛋白激酶抑制剂 A51 是一种强效的口服活性酪蛋白激酶 1α （CK1α）抑制剂。酪蛋白激酶抑制剂 A51 能诱导白血病细胞凋亡，具有强效抗白血病活性。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1C(=C(C=N1)C2=NC(=NC=C2Cl)NC3CCC(CC3)N)CC4CC4
PubChem CID
分子量
360.88
高级数据
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C of A & Other Certificates(BSE/TSE, COO):
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