2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. Dyrk1A-IN-5

Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research.

For research use only. We do not sell to patients.

Dyrk1A-IN-5 Chemical Structure

Dyrk1A-IN-5 Chemical Structure

CAS No. : 1685235-41-9

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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

Dyrk1A-IN-5 Related Antibodies

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View All DYRK Isoform Specific Products:

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DYRK1 DYRK2 DYRK3 DYRK4

  • Biological Activity

  • Purity & Documentation

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Description

Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research[1].

IC50 & Target

DYRK1A

6 nM (IC50)

DYRK1B

600 nM (IC50)

DYRK2

>10000 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.5 μM
Compound: 5j
Inhibition of DYRK1A in HEK293 cells assessed as inhibition of tau phosphorylation at Thr212 by Western blotting analysis
Inhibition of DYRK1A in HEK293 cells assessed as inhibition of tau phosphorylation at Thr212 by Western blotting analysis
[PMID: 25730262]
HeLa IC50
2.1 μM
Compound: 5j
Inhibition of DYRK1A in human HeLa cells assessed as reduction of SF3B1 phosphorylation by immunoblotting analysis
Inhibition of DYRK1A in human HeLa cells assessed as reduction of SF3B1 phosphorylation by immunoblotting analysis
[PMID: 25730262]
HT-22 IC50
> 100 μM
Compound: 7; Cpd 5j
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
[PMID: 36876904]
Molecular Weight

388.16

Formula

C16H9IN2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC2=CC=CC=C2C3=C1C4=C(N3)C(I)=CC=C4)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (8.58 mM; ultrasonic and warming and heat to 160°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5763 mL 12.8813 mL 25.7626 mL
5 mM 0.5153 mL 2.5763 mL 5.1525 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
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C2

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V2

In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
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 2.5763 mL 12.8813 mL 25.7626 mL 64.4064 mL
5 mM 0.5153 mL 2.5763 mL 5.1525 mL 12.8813 mL
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Dyrk1A-IN-5 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dyrk1A-IN-51685235-41-9DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseHeLa cellsHEK293 cellsDown syndromeAlzheimer’s diseaseInhibitorinhibitorinhibit

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