CLK1/2-IN-3

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CLK1/2-IN-3

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CAS NO:

1005784-60-0

CLK1/2-IN-3 (compound 3) 是一种有效的选择性CLK1和CLK2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。

生物活性

LK1/2-IN-3 (compound 3) is a potent and selectiveCLK1andCLK2inhibitor withIC₅₀values 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].

分子量

375.42

Formula

C₂₁H₂₁N₅O₂

CAS 号

1005784-60-0

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.