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. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC50 = 600 nM) and CLK1 (IC50 = 500 nM), but shows almost no inhibition of DYRK2 (IC50 > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research.

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

Dyrk1A-IN-5

Dyrk1A-IN-5 Chemical Structure

CAS No. : 1685235-41-9

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Dyrk1A-IN-5 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Dyrk1A-IN-5

View All DYRK Isoform Specific Products:

View All Isoforms
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

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Description

Dyrk1A-IN-5 (Compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC50 = 600 nM) and CLK1 (IC50 = 500 nM), but shows almost no inhibition of DYRK2 (IC50 > 10 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]
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]
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]
In Vitro

Dyrk1A-IN-5 (0-30 μM) dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM in Hela cells[1].
Dyrk1A-IN-5 (0-10 μM) inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM in HEK293 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dyrk1A-IN-5 Related Antibodies
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
Purity & Documentation
References
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Dyrk1A-IN-5 Related Classifications

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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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