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CK2/ERK8-IN-1 is a dual inhibitor of casein kinase 2 (CK2) (Ki 0.25 µM) and ERK8 (MAPK15, ERK7), both with IC50s of 0.50 µM. In addition, CK2/ERK8-IN-1 binds to PIM1, HIPK2, and DYRK1A with Ki values of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. 15.25 µM and 11.9 µM, respectively, and also has pro-apoptotic activity.
| Molecular Weight | 534.82 |
| Formula | C11H9Br4N3O2 |
| CAS Number | 1085822-09-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 16.67 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Guanfeng Wang, et al. J Plant Physiol. Casein kinase CK2 structure and activities in plants
[3] Scott E Roffey, et al. Biomedicines. CK2 Regulation: Perspectives in 2021
[4] Eduardo Silva-Pavez, et al. Front Oncol. Protein Kinase CK2 in Cancer Energetics
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| (R)-DRF053 dihydrochloride
(R)-DRF053 dihydrochloride is a potent inhibitor of casein kinase 1 (CK1), CDK1/cyclin B, and CDK5/p25, with IC50s of 14 nM, 220 nM, and 80 nM, respectively.(R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cellular models. In addition, (R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cell models. |
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