CK2-IN-9
CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC50 of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC50 of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat.
For research use only. We do not sell to patients.
- CAS No.: 1461658-58-1
- Formula: C23H29N9O
- Molecular Weight:447.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
4 μM
Compound: 7b
|
Inhibition of human ERG expressed in CHO cells by patch clamp assay
Inhibition of human ERG expressed in CHO cells by patch clamp assay
|
[PMID: 26985319] |
| DLD-1 | GI50 |
0.08 μM
Compound: 7b
|
Antiproliferative activity against human DLD1 cells after 72 hrs by alamar blue assay
Antiproliferative activity against human DLD1 cells after 72 hrs by alamar blue assay
|
[PMID: 26985319] |
| HCT-116 | GI50 |
0.03 μM
Compound: 7b
|
Antiproliferative activity against human HTC116 cells after 72 hrs by alamar blue assay
Antiproliferative activity against human HTC116 cells after 72 hrs by alamar blue assay
|
[PMID: 26985319] |
| HCT-116 | GI50 |
0.03 μM
Compound: Example 1
|
Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay
|
[PMID: 24900617] |
| Sf21 | IC50 |
<0.003 μM
Compound: 7b
|
Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay
Inhibition of full length N-terminal 6xHis-tagged recombinant human CK2alpha expressed in fall armyworm Sf21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate after 90 mins by mobility shift assay
|
[PMID: 26985319] |
| SW-620 | GI50 |
0.03 μM
Compound: 7b
|
Antiproliferative activity against human SW620 cells after 72 hrs by alamar blue assay
Antiproliferative activity against human SW620 cells after 72 hrs by alamar blue assay
|
[PMID: 26985319] |
Chemical Information
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CAS No. 1461658-58-1
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Molecular Weight 447.54
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Formula C23H29N9O
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SMILES
O=C(C)NC1=CC(NC2=NC3=C(C#N)C=NN3C(NC4CC4)=C2)=CC=C1N(CCN(C)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)