1. Cell Cycle/DNA Damage
  2. CDK SRPK
  3. CLK1/2-IN-3

CLK1/2-IN-3 (compound 3) 是一种有效的选择性 CLK1CLK2 抑制剂,CLK1、CLK2、SRPK1、SRPK2、SRPK3 的 IC50 值分别为 1.1、2.1、130、260、260 nM。CLK1/2-IN-3 显示出抗增殖活性。CLK1/2-IN-3 降低内源性磷酸化 SR 蛋白的水平并增加 S6K mRNA 的表达。

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CLK1/2-IN-3 Chemical Structure

CLK1/2-IN-3 Chemical Structure

CAS No. : 1005784-60-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs[1].

IC50 & Target[1]

CLK1

1.1 nM (IC50)

CLK2

2.1 nM (IC50)

SRPK1

130 nM (IC50)

SRPK2

260 nM (IC50)

SRPK3

260 nM (IC50)

体外研究
(In Vitro)

CLK1/2-IN-3 (compound 3) (1.1-3.3 μM; 72 h) increases the expression of S6K mRNAs in MDA-MB-468 cells[1].
CLK1/2-IN-3 (5 μM) significantly reduces the levels of endogenous phosphorylated SR proteins[1].
CLK1/2-IN-3 (1-10 μM) shows anti-proliferative activity with GI50s of 3.4, 2.6, 2.1, 2.5, 2.2, 2.9, 1.5 μM for MDA-MB-468, A549, COLO205, HCT-116, NCI-H23, SW620, COLO320DM cells, respectively[1].

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

分子量

375.42

Formula

C21H21N5O2

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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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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HY-113831
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