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Casein Kinase inhibitor A51

CAS No. : 2079068-74-7

MCE 站：Casein Kinase inhibitor A51

产品活性：Casein Kinase inhibitor A51 是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂。Casein Kinase inhibitor A51 可诱导白血病细胞凋亡 (apoptosis)，并具有有效的抗白血病活性。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Apoptosis

作用靶点：Casein Kinase  |  CDK  |  Apoptosis

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).

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).

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