| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
CKIδ
MU1742 targets three isoforms of casein kinase 1: CK1delta, CK1alpha, and CK1ε, with IC50 values of 6 nM, 7 nM, and 28 nM, respectively. It is highly selective for these isoforms and does not significantly inhibit other kinases. CK1 enzymes are involved in phosphorylation-mediated regulation of diverse cellular processes. |
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| ln Vitro |
MU1742 is a potent and highly selective inhibitor of CK1alpha, CK1delta, and CK1ε. It exhibits IC50 values of 6 nM for CK1delta, 7 nM for CK1alpha, and 28 nM for CK1ε. It is also orally bioavailable, making it suitable for in vivo studies. It represents the first potent and highly selective inhibitor of CK1alpha.
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| ln Vivo |
MU1742 inhibits CK1delta/ε-dependent DVL3 (Dishevelled-3) phosphorylation in mouse lung tissue, confirming target engagement in vivo. Its oral bioavailability enables convenient dosing in animal models for studying CK1-related pathologies such as cancer, neurodegenerative diseases, and circadian rhythm disorders.
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| Enzyme Assay |
A standard in vitro CK1 kinase inhibition assay involves incubating recombinant CK1delta, CK1alpha, or CK1ε enzyme (1-10 nM) with a specific peptide substrate (e.g., CK1tide: RRKDLHDDEEDEAMSITA) and ATP (10-100 microM) in kinase buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM DTT) with varying concentrations of MU1742 (0.1-1000 nM). The reaction proceeds for 30-60 minutes at 30degC, and phosphorylated peptide is quantified using a luminescent ADP detection kit (ADP-Glo) or by 33P-ATP incorporation. IC50 values are calculated by fitting dose-response curves.
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| Cell Assay |
A standard cellular protocol involves treating cells (e.g., HEK293 or cancer cell lines) with MU1742 at varying concentrations (0.01-10 microM) for 4-24 hours. After treatment, cells are lysed in RIPA buffer, and CK1 activity is assessed by Western blotting for phosphorylation levels of CK1 substrates such as DVL3 (p-DVL3), beta-catenin (p-beta-catenin at Ser45), or PER2. Target engagement is confirmed by dose-dependent reduction in substrate phosphorylation.
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| Animal Protocol |
A standard in vivo protocol involves administering MU1742 to mice by oral gavage (e.g., 1-10 mg/kg) or intraperitoneal injection. At various time points (1-8 hours post-dose), tissues (e.g., lung, liver, brain) are collected and lysed. CK1delta/ε-dependent DVL3 phosphorylation is measured by Western blotting using phospho-specific antibodies. Dose-dependent inhibition confirms target engagement in vivo, and pharmacokinetic parameters (Cmax, T1/2) can be determined from plasma samples.
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| ADME/Pharmacokinetics |
MU1742 is orally bioavailable with good absorption and distribution. Its molecular formula is C22H22F2N6, molecular weight 408.45 (free base), and purity ≥98%. It is soluble in DMSO for in vitro studies. For oral administration, it can be formulated in 0.5% methylcellulose or other suitable vehicles. Detailed PK parameters (half-life, bioavailability, volume of distribution) are not provided in the literature.
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| Toxicity/Toxicokinetics |
No specific toxicological data for MU1742 is available in the literature. As a selective CK1 inhibitor, its toxicity profile is expected to be related to the physiological roles of CK1 enzymes, which include regulation of the circadian clock, Wnt signaling, membrane trafficking, and DNA repair. Off-target effects are minimized due to its high isoform selectivity.
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| References | |
| Additional Infomation |
MU1742 is a research-grade selective CK1 inhibitor. It represents a significant advance as the first potent and highly selective inhibitor of CK1alpha. Its 1H-pyrrolo[2,3-b]pyridine-imidazole pharmacophore serves as a scaffold for developing inhibitors of other protein kinases (e.g., p38alpha). It has not been approved for clinical use and is strictly for laboratory research in cancer biology, circadian rhythm studies, and neurodegenerative diseases.
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| Molecular Formula |
C22H22F2N6
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|---|---|
| Molecular Weight |
408.45
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| Appearance |
White to off-white solid powder
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| SMILES |
CN1CCC(CN2C=NC(C3=NC=C(C=C3)F)=C2C4=CC=NC5=C4C=CN5)(CC1)F
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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: ~100 mg/mL (~244.8 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.12 mM) 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; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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. Solubility in Formulation 2: 2.5 mg/mL (6.12 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (6.12 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4483 mL | 12.2414 mL | 24.4828 mL | |
| 5 mM | 0.4897 mL | 2.4483 mL | 4.8966 mL | |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4483 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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