性能参数

产品名称

Casein Kinase inhibitor A51

规格

5 mg

货号

GOY-Y2185

 含量

>98.00%

CAS

2079068-74-7

别名

N/A

化学名

N/A

分子式

C18H25ClN6

分子量

分子 360.88

溶解度

N/A

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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[1]. 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[1].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)[1].

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[1].Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A51 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.5-2 hr, Cmax of 1060 ng/mL, T1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL)[1].

[1]. Waleed Minzel, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.

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异氰酸丙基三乙氧基硅烷 95%  (S)-4-氯-3-羟基丁酸乙酯  96%

碳酸亚乙烯酯 包含 <2% BHT稳定剂,98%  4-氯丁酸甲酯  98%

N-(叔丁氧羰基)-D-赖氨酸  98%  3,3-二甲基-1-丁炔 95%

硅酸钾 AR,K2CIO3 47-51%  2,3-二氢呋喃 99%

2-乙基-4-甲基咪唑 96%  双环丙基酮 95%

2-乙基-4-甲基咪唑 99%  1,2-二氯丙烷 99%

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