1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    Apoptosis
  2. Casein Kinase
    CDK
    Apoptosis
  3. Casein Kinase inhibitor A86

Casein Kinase inhibitor A86 

Cat. No.: HY-123955
Handling Instructions

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.

For research use only. We do not sell to patients.

Casein Kinase inhibitor A86 Chemical Structure

Casein Kinase inhibitor A86 Chemical Structure

CAS No. : 2079069-01-3

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Description

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].

IC50 & Target[1]

CKIα

 

CDK7

0.31 nM (Kd)

CDK9

5.4 nM (Kd)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

344.43

Formula

C₁₈H₂₅FN₆

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Casein Kinase inhibitor A86
Cat. No.:
HY-123955
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