| Targets |
Casein kinase 1δ[1].
Casein kinase 1δ-IN-7 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 Alzheimer’s disease and other tauopathies. Inhibition of CK1δ is a therapeutic strategy for neurodegenerative diseases. |
|---|---|
| ln Vitro |
In vitro activity data for Casein kinase 1δ-IN-7 are not extensively detailed in the available literature. As a CK1δ inhibitor, it is expected to inhibit CK1δ kinase activity in biochemical assays. The compound is used in cell-based studies to assess its effects on CK1δ-dependent signaling pathways and tau phosphorylation. Further in vitro studies are needed to determine its precise potency and selectivity profile.
|
| ln Vivo |
In vivo activity data for Casein kinase 1δ-IN-7 are not extensively documented. As a CK1δ inhibitor, it is expected to exhibit activity in animal models of neurodegenerative diseases. The compound may be used to study the effects of CK1δ inhibition on tau pathology, neuroinflammation, and cognitive function in vivo. Comprehensive in vivo studies are needed to fully characterize its efficacy and safety profile.
|
| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cell-based) assay for Casein kinase 1δ-IN-7 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, fluorescence-based assays, or ELISA. The compound’s IC50 value is determined from dose-response curves.
|
| Cell Assay |
The in vitro cell-based assay for Casein kinase 1δ-IN-7 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. Cellular effects such as changes in circadian rhythm or Wnt signaling may also be measured. The compound’s effects on tau phosphorylation are of particular interest for Alzheimer’s disease research.
|
| Animal Protocol |
In vivo animal experiments for Casein kinase 1δ-IN-7 are conducted in models of neurodegenerative diseases such as 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.
|
| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of Casein kinase 1δ-IN-7 are not extensively reported. The compound has a molecular weight of 338.38 g/mol and a molecular formula of C17H14N4O2S. It is soluble in DMSO (55 mg/mL, 162.54 mM). The compound is typically stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. Further pharmacokinetic studies are needed.
|
| Toxicity/Toxicokinetics |
Toxicological data for Casein kinase 1δ-IN-7 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.
|
| References | |
| Additional Infomation |
Casein kinase 1δ-IN-7 (CAS 764694-25-9) is an inhibitor of casein kinase 1δ used for the study of neurodegenerative diseases such as Alzheimer’s disease. It has a molecular weight of 338.38 g/mol and a formula of C17H14N4O2S. The compound is also known as compound 497. It is not approved for clinical use and is available only for research purposes. Purity is ≥98.02%.
|
| Exact Mass |
338.083
|
|---|---|
| CAS # |
764694-25-9
|
| PubChem CID |
2082307
|
| Appearance |
White to light yellow solid powder
|
| LogP |
3.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
24
|
| Complexity |
508
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PYESIJQNFOYDTC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H14N4O2S/c1-10-11(2)24-17-15(10)16(19-9-20-17)23-8-14(22)21-13-5-3-4-12(6-13)7-18/h3-6,9H,8H2,1-2H3,(H,21,22)
|
| Chemical Name |
N-(3-cyanophenyl)-2-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)oxyacetamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
