1. Protein Tyrosine Kinase/RTK
  2. DYRK
  3. 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 화학구조

CAS No. : 1685235-41-9

사이즈 가격 재고 수량
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Dyrk1A-IN-5

View All DYRK Isoform Specific Products:

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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.

분자량

388.16

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
순도&문서
References
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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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.

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상품명:
Dyrk1A-IN-5
Cat. No.:
HY-146221
수량:
MCE Japan Authorized Agent: