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

Dyrk1A-IN-5 (Compound 5j) 是一种强效且选择性的 DYRK1A 抑制剂，其 IC50 值为 6 nM。Dyrk1A-IN-5 对DYRK1B (IC50 = 600 nM) 和CLK1 (IC50 = 500 nM) 具有显著选择性，对DYRK2 (IC50 > 10 μM) 几乎无抑制。Dyrk1A-IN-5 可用于唐氏综合征的研究。

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Dyrk1A-IN-5

Dyrk1A-IN-5 Chemical Structure

CAS No. : 1685235-41-9

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规格 价格 是否有货 数量
1 mg ￥1454
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5 mg ￥3200
In-stock
10 mg ￥5100
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Dyrk1A-IN-5 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 DYRK 亚型特异性产品:

查看所有亚型
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(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]
体外研究
(In Vitro)

Dyrk1A-IN-5 (0-30 μM) 以剂量依赖的方式降低 SF3B1 中 Thr434 位点的磷酸化水平，在 HeLa 细胞中 IC50 为 0.5 μM[1]。
Dyrk1A-IN-5 (0-10 μM) 抑制 tau 蛋白 Thr212 位点的磷酸化，在 HEK293 细胞中 IC50 为 2.1 μM[1]。

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

Dyrk1A-IN-5 相关抗体:
分子量

388.16

Formula

C16H9IN2O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

Dyrk1A-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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