| Identification | Back Directory | [Name]
Casein Kinase inhibitor A86 | [CAS]
2079069-01-3 | [Synonyms]
CKIα inhibitor A86
Casein Kinase inhibitor A86
1,4-Cyclohexanediamine, N1-[4-[5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl]-5-fluoro-2-pyrimidinyl]-, trans- | [Molecular Formula]
C18H25FN6 | [MOL File]
2079069-01-3.mol | [Molecular Weight]
344.43 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 12.5 mg/mL (36.29 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
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[1].
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].
Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.2-0.5 hr, Cmax of 1115 ng/mL, T1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL)[1]. | [in vivo]
Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.2-0.5 hr, Cmax of 1115 ng/mL, T1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL)[1]. | [IC 50]
CKIα; CDK7: 0.31 nM (Kd); CDK9: 5.4 nM (Kd) | [References]
[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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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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