| Size | Price | Stock | Qty |
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| 100mg |
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| Targets |
CKIδ
Casein kinase 1δ-IN-1 targets casein kinase 1δ (CK1δ), a serine/threonine protein kinase involved in various cellular processes including circadian rhythm regulation, Wnt signaling, and neurodegenerative disease pathogenesis. CK1δ has been implicated in the hyperphosphorylation of tau protein, a hallmark of tauopathies and Alzheimer’s disease. Inhibition of CK1δ is a therapeutic strategy for neurodegenerative diseases. |
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| ln Vitro |
In vitro activity data for Casein kinase 1δ-IN-1 indicate that it is an inhibitor of CK1δ with inhibitory activity greater than 5%. As a CK1δ inhibitor, it is expected to inhibit CK1δ kinase activity in biochemical assays and reduce tau phosphorylation in cell-based systems. Further in vitro studies are needed to determine its precise IC50 value and selectivity profile.
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| ln Vivo |
In vivo activity data for Casein kinase 1δ-IN-1 are not extensively documented. As a CK1δ inhibitor, it is expected to exhibit activity in animal models of neurodegenerative diseases such as tauopathies and Alzheimer’s disease. The compound may be used to study the effects of CK1δ inhibition on tau pathology and cognitive function in vivo. Comprehensive in vivo studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cell-based) assay for Casein kinase 1δ-IN-1 involves assessing its inhibition of CK1δ kinase activity. Recombinant CK1δ is incubated with the compound, ATP, and a substrate peptide. Kinase activity is measured by detecting phosphorylated substrate using techniques such as radiometric assays or fluorescence-based assays. The compound’s IC50 value is determined from dose-response curves.
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| Cell Assay |
The in vitro cell-based assay for Casein kinase 1δ-IN-1 involves treating cells with the compound and measuring CK1δ-dependent signaling and functional responses. Cells expressing CK1δ are treated with the compound, and downstream phosphorylation of CK1δ substrates (e.g., tau protein) is assessed by Western blotting or ELISA. The compound’s effects on tau phosphorylation are of particular interest for neurodegenerative disease research.
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| Animal Protocol |
In vivo animal experiments for Casein kinase 1δ-IN-1 are conducted in models of neurodegenerative diseases such as tauopathies and Alzheimer’s disease. Animals are administered the compound via appropriate routes, and disease progression is monitored through behavioral tests, histopathological analysis (e.g., tau pathology), and measurement of neuroinflammatory markers. The compound’s ability to inhibit CK1δ and reduce tau phosphorylation in vivo is assessed.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of Casein kinase 1δ-IN-1 are not extensively reported. The compound has a molecular formula of C11H7N3OS. Further pharmacokinetic studies are needed to determine its half-life, bioavailability, and brain penetration. The compound is typically used for research purposes only.
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| Toxicity/Toxicokinetics |
Toxicological data for Casein kinase 1δ-IN-1 are not extensively documented. As a research compound, its safety profile is evaluated in standard cytotoxicity and acute toxicity assays. The compound is classified for research use only and is not intended for human therapeutic use. Comprehensive toxicological characterization would be required prior to any clinical development.
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| References | |
| Additional Infomation |
Casein kinase 1δ-IN-1 (CAS 851871-94-8) is an inhibitor of casein kinase 1δ (CK1δ) used for the research of neurodegenerative diseases such as tauopathies and Alzheimer’s disease. It has a molecular formula of C11H7N3OS. The compound is also known as WAY-643895. It is not approved for clinical use and is available only for research purposes. Purity is ≥99.91%.
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| Molecular Formula |
C11H7N3OS
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|---|---|
| Molecular Weight |
229.257780313492
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| Exact Mass |
229.03
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| CAS # |
851871-94-8
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| PubChem CID |
2525612
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| Appearance |
Off-white to light brown solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
312
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#CC1=C(NC(C2C=CC=CN=2)=O)SC=C1
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| InChi Key |
XNEHUAKGYXQSBF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H7N3OS/c12-7-8-4-6-16-11(8)14-10(15)9-3-1-2-5-13-9/h1-6H,(H,14,15)
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| Chemical Name |
N-(3-cyanothiophen-2-yl)pyridine-2-carboxamide
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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: 41.67 mg/mL (181.76 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3619 mL | 21.8093 mL | 43.6186 mL | |
| 5 mM | 0.8724 mL | 4.3619 mL | 8.7237 mL | |
| 10 mM | 0.4362 mL | 2.1809 mL | 4.3619 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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