| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
IC50: 2.3 nM (CSNK1D)[2]
JNJ-6204 targets casein kinase 1 delta (CSNK1D) and casein kinase 1 epsilon (CSNK1E). These are serine/threonine kinases belonging to the CK1 family, which regulate various biological processes including circadian rhythm, Wnt signaling, and membrane trafficking. JNJ-6204 potently inhibits CSNK1D with an IC50 of 2.3 nM and CSNK1E with an IC50 of 137 nM. |
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| ln Vitro |
In the BRET whole cell binding test and the PER2 translocation whole cell functional assay, JNJ-6204 suppresses CSNK1D with IC50 values of 72 nM and 542 nM, respectively[2].
In vitro, JNJ-6204 potently inhibits CSNK1D with an IC50 of 2.3 nM and CSNK1E with an IC50 of 137 nM. In whole-cell assays, it inhibits CSNK1D in the BRET binding assay and the PER2 translocation functional assay with IC50s of 72 nM and 542 nM, respectively. It shows good brain penetration, making it valuable for studying neurological functions of CK1 kinases. |
| ln Vivo |
In vivo data for JNJ-6204 is limited in publicly available sources. As a brain-penetrant dual inhibitor of CSNK1D and CSNK1E, the compound has potential applications in animal models of circadian rhythm disorders, neurodegenerative diseases, and cancer. However, specific published in vivo efficacy studies are not detailed in the current literature. JNJ-6204 is primarily used as a research tool for studying CK1 kinase biology.
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| Enzyme Assay |
The in vitro CK1 inhibition assay for JNJ-6204 uses recombinant CSNK1D and CSNK1E enzymes and a peptide substrate. Kinase activity is measured using radioactive or luminescent detection methods, and IC50 values are calculated from dose-response curves. Whole-cell assays, such as the BRET binding assay and PER2 translocation assay, are used to assess cellular potency. Selectivity is confirmed by profiling against a panel of kinases.
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| Cell Assay |
Cellular assays for JNJ-6204 are conducted in relevant cell lines. The compound's cellular potency is assessed using the BRET whole-cell binding assay and the PER2 translocation functional assay, with IC50s of 72 nM and 542 nM, respectively. The effects on CK1 signaling pathways, such as Wnt signaling and circadian rhythm regulation, are evaluated using reporter gene assays or by measuring downstream target phosphorylation.
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| Animal Protocol |
In vivo studies for JNJ-6204 would typically involve animal models of circadian rhythm disorders, neurodegenerative diseases, or cancer. The compound would be administered via oral or intraperitoneal routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring behavioral, neurological, or tumor-related endpoints. However, specific published in vivo protocols for JNJ-6204 are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for JNJ-6204 indicates that it has good brain penetration, making it suitable for studying neurological targets. The compound has a molecular weight of 389.5 g/mol. As a small molecule, it is expected to have moderate oral bioavailability. Detailed PK parameters such as half-life and bioavailability are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Toxicity data for JNJ-6204 is limited in publicly available sources. As with all research compounds, JNJ-6204 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. The compound's selectivity profile against a panel of 370 kinases at 1 μM appears clean.
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| References |
[1]. Terry Patrick LEBOLD, et al. Casein kinase 1 delta modulators. WO2022058920A1. [2]. https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/JNJ-6204
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| Additional Infomation |
JNJ-6204 (CAS 2765264-50-2) is a potent, brain-penetrant dual inhibitor of CSNK1D (IC50 = 2.3 nM) and CSNK1E (IC50 = 137 nM). It is a valuable research tool for studying circadian rhythm regulation, Wnt signaling, and neurodegenerative diseases. It shows good brain exposure and has a clean selectivity profile against a panel of 370 kinases at 1 μM.
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| CAS # |
2765264-50-2
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|---|---|
| Appearance |
Typically exists as solid at room temperature
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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) |
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
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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.) |
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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