| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C11H14Cl3N3O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1), with an IC50 of 6 μM and a Ki of 8.5 μM, and it also selectively inhibits Cdc7 kinase. It additionally inhibits SGK, ribosomal S6 kinase-1 (S6K1), and mitogen- and stress-activated protein kinase-1 (MSK1), while having a much weaker effect on casein kinase II and other protein kinases[1][2][3][4]. It is supplied as a light yellow to yellow solid (C11H14Cl3N3O2S, MW 358.67) at 99.97% purity.
Physical & Chemical Properties
| CAS Number | 1177141-67-1 |
|---|---|
| Molecular Formula | C11H14Cl3N3O2S |
| Molecular Weight | 358.67 g/mol |
| Purity | 99.97% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=S(C1=CC=C(Cl)C2=C1C=NC=C2)(NCCN)=O.[H]Cl.[H]Cl |
| Target | CK1, p70S6K, Cdc7, SGK, MSK1 |
| Signaling Pathway | Cell Cycle/DNA Damage; Stem Cell/Wnt; Metabolic Enzyme/Protease; MAPK/ERK Pathway |
| Solubility | In Vitro: H2O: 10 mg/mL (27.88 mM; Requires sonication and warming and heat to 60°C) DMSO: 5 mg/mL (13.94 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
[1][2][3]
|
CK1 6 μM (IC50) |
CK1 8.5 μM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[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.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | 10 mg/mL (27.88 mM) | requires sonication and warming and heat to 60°C |
| DMSO | 5 mg/mL (13.94 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
Data provided by the manufacturer.
In Vitro
CKI-7 (0.1-10 μM; 5 days; ES cells) treatment significantly increases, in a concentration-dependent manner, expression of the early neuroectodermal marker Sox1 and the count of cells positive for nestin and βIII-tubulin (neural markers)[1]. Under CKI-7 treatment (5 μM; 5 days; ES cells), SFEB-induced β-catenin stabilization is suppressed on day 5, showing that CKI-7 inhibits Wnt signaling[1].
RT-PCR[1]
| Cell Line | Mouse ES cells |
|---|---|
| Concentration | 0.1-10 μM |
| Incubation Time | 5 days |
| Result | Significantly increased the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner. |
Western Blot Analysis[1]
| Cell Line | Mouse ES cells |
|---|---|
| Concentration | 5 μM |
| Incubation Time | 5 days |
| Result | Suppressed SFEB-induced β-catenin stabilization on day 5. |
In Vivo
CKI-7 shows dose-dependent anti-tumor activity in vivo in a SCID-Beige mouse systemic tumor model using a Philadelphia chromosome positive acute lymphoblastic leukemia cell line isolated recently. In standard cell cycle synchronization studies, exposure to CKI-7 leads to cell cycle dependent caspase 3 activation and apoptotic cell death[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Phosphorylation-dependent allosteric regulation of Cx43 gap junction inhibitor potency. Biomed Pharmacother 2024 May:174:116550. PMID: 38593702
