1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK
  2. CDK DYRK
  3. Leucettinib-92

Leucettinib-92 (compound 92) 是 DYRK/CLK 激酶的抑制剂,IC50s 分别为 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)。

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Leucettinib-92 Chemical Structure

Leucettinib-92 Chemical Structure

CAS No. : 2732859-57-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)[1].

IC50 & Target

IC50: 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-22 IC50
6.3 μM
Compound: 22
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]
体外研究
(In Vitro)

Leucettinib-92 (0.1-10 μM; 3 min) 与 SH-SY5Y 细胞中的 DYRK1A 结合,诱导其稳定直到 52°C 以上的熔化温度。Leucettinib-92 (1 μM) 抑制 2 种 DYRK1A 底物 (Thr212-Tau and Thr286-cyclin D1) 的磷酸化[1]

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

分子量

378.49

Formula

C21H22N4OS

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • 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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产品名称:
Leucettinib-92
目录号:
HY-155723
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