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.

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Dyrk1A-IN-5

Dyrk1A-IN-5 構造式

CAS 番号 : 1685235-41-9

容量 価格（税別） 在庫状況 数量
5 mg $320 在庫あり
10 mg $510 在庫あり
25 mg $1050 在庫あり
50 mg $1680 在庫あり
100 mg $2650 在庫あり
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Based on 1 publication(s) in Google Scholar

Dyrk1A-IN-5 関連抗体

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DYRK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

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製品説明

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]
体外実験

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 関連抗体
分子量

388.16

分子式

C16H9IN2O2
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC2=CC=CC=C2C3=C1C4=C(N3)C(I)=CC=C4)O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
純度とドキュメンテーション
参考文献
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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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製品名:
Dyrk1A-IN-5
製品番号:
HY-146221
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