DYRK2-IN-2 hydrochloride
Based on 1 Customer Validation
DYRK2-IN-2 hydrochloride is a selective DYRK2 inhibitor with an IC50 of 40.3 nM. DYRK2-IN-2 hydrochloride shows weaker inhibitory activity against DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM) and CLK (IC50 = 540-6496 nM). DYRK2-IN-2 hydrochloride inhibits the phosphorylation of Thr212 in Tau protein. DYRK2-IN-2 hydrochloride is applicable for neuronal research.
For research use only. We do not sell to patients.
- Formula: C21H25ClN2O3S
- Molecular Weight:420.95
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Storage:Powder -20°C, 3 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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Biological Activity
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DYRK2 40.3 nM (IC50) |
DYRK1A 1842 nM (IC50) |
DYRK1B 1335 nM (IC50) |
DYRK4 1931 nM (IC50) |
DYRK3 112 nM (IC50) |
CLK1 1128 nM (IC50) |
CLK2 4290 nM (IC50) |
CLK3 6496 nM (IC50) |
CLK4 536.9 nM (IC50) |
DYRK2-IN-3 (Compound C17) (up to 10 μM) hydrochloride potently and selectively inhibits recombinant DYRK2 with an IC50 of 0.0403 μM; it shows weak activity against other kinases of the DYRK and CLK families, and no activity against CDK5/p25, CK1ε or GSK3β[1].
DYRK2-IN-3 (1-30 μM; 6 h) hydrochloride potently and dose-dependently inhibits Thr212-Tau phosphorylation in SH-SY5Y cells expressing 4R-Tau[1].
DYRK2-IN-3 (48 h) hydrochloride exhibits cytotoxicity against HT22 cells, with an IC50 of 14.7 μM following 48 h of exposure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells expressing human 4R-Tau
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Concentration:1-30 μM
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Incubation Time:6 h
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Result:Efficiently and dose-dependently inhibited phosphorylation of Tau at the Thr212 site.
Induced a distinct second band in total Tau staining at the highest tested concentration.
Chemical Information
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Appearance Solid
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Molecular Weight 420.95
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Formula C21H25ClN2O3S
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SMILES
COC1=CC2=C(SC[C@H]3CCNC3)C4=C(N=C2C=C1)C(CO)=CC(OC)=C4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (59.39 mM; Need ultrasonic; 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)
Purity & Documentation
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 | 2.3756 mL | 11.8779 mL | 23.7558 mL | 59.3895 mL |
| 5 mM | 0.4751 mL | 2.3756 mL | 4.7512 mL | 11.8779 mL | |
| 10 mM | 0.2376 mL | 1.1878 mL | 2.3756 mL | 5.9389 mL | |
| 15 mM | 0.1584 mL | 0.7919 mL | 1.5837 mL | 3.9593 mL | |
| 20 mM | 0.1188 mL | 0.5939 mL | 1.1878 mL | 2.9695 mL | |
| 25 mM | 0.0950 mL | 0.4751 mL | 0.9502 mL | 2.3756 mL | |
| 30 mM | 0.0792 mL | 0.3959 mL | 0.7919 mL | 1.9796 mL | |
| 40 mM | 0.0594 mL | 0.2969 mL | 0.5939 mL | 1.4847 mL | |
| 50 mM | 0.0475 mL | 0.2376 mL | 0.4751 mL | 1.1878 mL |
DYRK2-IN-2 hydrochloride Related Classifications
HY-402805A Related Classifications
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