DYRK1-IN-1
Based on 3 publication(s) in Google Scholar
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 2814486-79-6
- Formula: C12H12N6
- Molecular Weight:240.26
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DYRK1-IN-1
More
Biological Activity
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DYRK1A 220 nM (IC50) |
DYRK1A 3 nM (Kd) |
DYRK1B 56 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-22 | IC50 |
58.6 μM
Compound: 36; Cpd 11
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 inhibits tau phosphorylation with an IC50 value of 0.59 μM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability. DYRK1-IN-1 has good physicochemical properties and has demonstrated high levels of enzymatic potency, favorable aqueous solubility, exquisite kinome selectivity, and promising on-target in vitro inhibition. DYRK1-IN-1 (HEK293 cells) demonstrates acceptable cellular activity, with IC50 of 434 nM compared to the enzymatic IC50 of 75 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague−Dawley rats[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:I.v.
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Result:High clearance was observed.
Chemical Information
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CAS No. 2814486-79-6
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Appearance Solid
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Molecular Weight 240.26
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Formula C12H12N6
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Color White to off-white
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SMILES
CN(C1=NC(C2=C3C=CC=NN3N=C2)=CC=N1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Mol Biol Lett
2023 Jul 27;28(1):60. PMID: 37501148 -
EMBO J
2024 Oct;43(20):4752-4785. PMID: 39256562 -
J Integr Neurosci
Harmine-mediated Reduction of Bone Cancer Pain in Rats Correlates With Suppressed DYRK1A/NF-κB Signaling Axis. [Abstract]2025 Jun 23;24(6):38100. PMID: 40613372
Solvent & Solubility
DMSO : 25 mg/mL (104.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.1622 mL | 20.8108 mL | 41.6216 mL | 104.0539 mL |
| 5 mM | 0.8324 mL | 4.1622 mL | 8.3243 mL | 20.8108 mL | |
| 10 mM | 0.4162 mL | 2.0811 mL | 4.1622 mL | 10.4054 mL | |
| 15 mM | 0.2775 mL | 1.3874 mL | 2.7748 mL | 6.9369 mL | |
| 20 mM | 0.2081 mL | 1.0405 mL | 2.0811 mL | 5.2027 mL | |
| 25 mM | 0.1665 mL | 0.8324 mL | 1.6649 mL | 4.1622 mL | |
| 30 mM | 0.1387 mL | 0.6937 mL | 1.3874 mL | 3.4685 mL | |
| 40 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 50 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0811 mL | |
| 60 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7342 mL | |
| 80 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 100 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0405 mL |
DYRK1-IN-1 Related Classifications
HY-132308 Related Classifications
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