| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Casein Kinase II Inhibitor IV targets casein kinase II (CK2), a serine/threonine protein kinase involved in cell proliferation, survival, and differentiation; it competitively inhibits CK2 at the ATP-binding site with high potency (IC50 = 9 nM).
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| ln Vitro |
After 48 hours, the early differentiation markers keratin 1 and 10 were upregulated in human epidermal keratinocytes (NHEK) treated with casein kinase II inhibitor IV. Cells treated with IV casein kinase II inhibitor showed increased levels of IVL and TGM for 72 hours, and these levels continued for 96 hours. Additionally, at later times, treatment with casein kinase II inhibitor IV led to the production of loricrin, a hallmark of final differentiation. When NHEK was treated with casein kinase II inhibitor IV, messenger RNA (mRNA) expression study revealed similar outcomes. Treatment with casein kinase II inhibitor IV upregulated keratinocyte early differentiation marker genes, such as keratin 1 (5.4-fold) and keratin 10 (5.4-fold), at early time points (12 and 24 hours). At later times (36 and 48 hours), there was an upregulation of terminal differentiation marker genes, such as IVL (1.8-fold), TGM 1 (4.8-fold), loricrin (3.3-fold), and filaggrin (5.6-fold). These findings confirm that casein kinase II inhibitor IV can stimulate epidermal progenitor cells to develop into terminally differentiated keratinocytes [1].
In vitro kinase assays demonstrate that Casein Kinase II Inhibitor IV potently inhibits CK2 activity with an IC50 of 9 nM; treatment of human epidermal keratinocytes (NHEKs) enhances early differentiation markers including keratins 1 and 10 at 48 hours, and increases levels of involucrin (IVL) and transglutaminase (TGM) at 72 hours, sustained through 96 hours. |
| ln Vivo |
In vivo, Casein Kinase II Inhibitor IV has been used to study the role of CK2 in epidermal differentiation and other biological processes, though detailed in vivo efficacy data are primarily derived from in vitro and ex vivo studies; it serves as a tool for investigating CK2 function in differentiation and disease.
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| Enzyme Assay |
The in vitro kinase assay for CK2 inhibition involves incubating Casein Kinase II Inhibitor IV with recombinant human CK2 enzyme and a peptide substrate (e.g., a synthetic CK2 substrate) in the presence of ATP, measuring phosphorylation via scintillation counting of incorporated 32P or by fluorescence-based detection using labeled phospho-substrate antibodies, with IC50 values calculated from concentration-response curves.
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| Cell Assay |
In vitro cell culture studies utilize human epidermal keratinocytes (NHEKs) treated with Casein Kinase II Inhibitor IV, assessing differentiation markers by Western blotting (keratins 1 and 10, involucrin, transglutaminase) and immunofluorescence staining, cell proliferation by BrdU incorporation, and CK2 activity by measuring phosphorylation of endogenous substrates.
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| Animal Protocol |
In vivo animal experiments for studying CK2 inhibition and keratinocyte differentiation involve topical or systemic administration of Casein Kinase II Inhibitor IV to mouse models of skin diseases (e.g., psoriasis, wound healing), followed by histopathological analysis of skin tissues, assessment of differentiation markers by immunohistochemistry, and evaluation of epidermal thickness and barrier function.
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| ADME/Pharmacokinetics |
Casein Kinase II Inhibitor IV has a molecular weight of approximately 450 g/mol and purity of ≥95.7%; it is a cell-permeable compound stored as a powder at -20°C, soluble in DMSO, and should be protected from light and moisture.
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| Toxicity/Toxicokinetics |
Toxicological data for Casein Kinase II Inhibitor IV are limited to in vitro cytotoxicity assessments; as a kinase inhibitor, it may have off-target effects at higher concentrations, and comprehensive in vivo toxicity studies have not been extensively reported for this research compound.
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| References | |
| Additional Infomation |
Casein Kinase II Inhibitor IV is a research compound used for studying CK2 biology, keratinocyte differentiation, and the therapeutic potential of CK2 inhibition in skin disorders and cancer; it has not been approved for clinical use and serves as a valuable tool for investigating CK2-mediated signaling pathways.
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| Molecular Formula |
C24H23N5O3
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|---|---|
| Molecular Weight |
429.47112
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| Exact Mass |
429.18
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| CAS # |
863598-09-8
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| Related CAS # |
Casein Kinase II Inhibitor IV hydrochloride;2320347-54-2
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| PubChem CID |
11453158
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.719
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
628
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KKVZKYOBQGDKIB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23N5O3/c1-30-20-13-18(14-21(31-2)22(20)32-3)27-24-26-15-17-9-11-29(23(17)28-24)19-8-4-6-16(12-19)7-5-10-25/h4,6,8-9,11-15H,5,7H2,1-3H3,(H,26,27,28)
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| Chemical Name |
3-[3-[2-(3,4,5-trimethoxyanilino)pyrrolo[2,3-d]pyrimidin-7-yl]phenyl]propanenitrile
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~77.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3285 mL | 11.6423 mL | 23.2845 mL | |
| 5 mM | 0.4657 mL | 2.3285 mL | 4.6569 mL | |
| 10 mM | 0.2328 mL | 1.1642 mL | 2.3285 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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