| Description | CKI-7 free base is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1. |
| In vitro | The treatment of CKI-7 (0.1-10 μM; 5 days; ES cells) significantly increases the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers βIII-tubulin and nestin, in a concentration-dependent manner. CKI-7 (5 μM; 5 days; ES cells) treatment suppresses SFEB-induced β-catenin stabilization on day 5 [1]. |
| In vivo | In vivo dose-dependent, the anti-tumor activity of CKI-7 is demonstrated in a SCID-Beige mouse systemic tumor model utilizing isolated Philadelphia chromosome-positive acute lymphoblastic leukemia cell line. Exposure to CKI-7 results in a cell cycle-dependent caspase 3 activation and apoptotic cell death [2]. |
| Target activity | CK1:6 μM, CK1:8.5 μM (ki) |
| Synonyms | CKI-7 |
| molecular weight | 285.75 |
| Molecular formula | C11H12ClN3O2S |
| CAS | 120615-25-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (87.49 mM), Sonication is recommended. |
| References | 1. Osakada F, et al. In vitro differentiation of retinal cells from human pluripotent stem cells by small-molecule induction. J Cell Sci. 2009 Sep 1;122(Pt 17):3169-79. 2. Mark G. Frattini, et al. Small Molecule Inhibition of Cdc7, a Key Cell Cycle Regulator and Novel Therapeutic Target, Successfully Inhibits Leukemia Cell Growth in Vitro and in Vivo. Blood (2008) 112 (11): 2668. 3. Chijiwa T, et al. A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis. J Biol Chem. 1989 Mar 25;264(9):4924-7. 4. Rena G, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5. |