| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C11H12ClN3O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CKI-7 free base is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1), with an IC50 of 6 μM and a Ki of 8.5 μM. It is also a selective inhibitor of Cdc7 kinase and 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 an off-white to light yellow solid (C11H12ClN3O2S, MW 285.75) at 99.31% purity.
Physical & Chemical Properties
| CAS Number | 120615-25-0 |
|---|---|
| Molecular Formula | C11H12ClN3O2S |
| Molecular Weight | 285.75 g/mol |
| Purity | 99.31% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | O=S(C1=CC=C(Cl)C2=C1C=NC=C2)(NCCN)=O |
| Target | CK1, p70S6K, Cdc7, SGK, MSK1 |
| Signaling Pathway | Cell Cycle/DNA Damage; Stem Cell/Wnt; Metabolic Enzyme/Protease; MAPK/ERK Pathway |
| Solubility | In Vitro: DMSO: 25 mg/mL (87.49 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| 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 |
|---|---|---|
| DMSO | 25 mg/mL (87.49 mM) | requires sonication; 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); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (7.28 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (7.28 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (7.28 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In ES cells, CKI-7 (0.1-10 μM; 5 days) causes a concentration-dependent, significant rise in Sox1 expression, an early neuroectodermal marker, and in the number of cells positive for nestin and βIII-tubulin, which are neural markers[1]. In ES cells, CKI-7 (5 μM; 5 days) reduces SFEB-induced stabilization of β-catenin on day 5, which indicates 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 that uses a Philadelphia chromosome positive acute lymphoblastic leukemia cell line, recently isolated. Standard cell cycle synchronization studies show that CKI-7 exposure 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
