10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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
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. 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). 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
Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a T max of 0.2-0.5 hr, C max of 1115 ng/mL, T 1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:CKIα CDK7 0.31 nM (Kd) CDK9 5.4 nM (Kd)
| Molecular Weight | 344.43 |
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