CLK1/2-IN-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

CLK1/2-IN-3 (compound 3) (1.1-3.3 μM; 72 h) increases the expression of S6K mRNAs in MDA-MB-468 cells.CLK1/2-IN-3 (5 μM) significantly reduces the levels of endogenous phosphorylated SR proteins.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.

——

——

Cell Cycle/DNA Damage

CDK

CDK

——

——

1005784-60-0

375.42

C21H21N5O2

>98% (HPLC)

——

N(C(=O)C1=CC=C(C(CO)(C)C)C=C1)C2=CN3C(=N2)C=CC(=C3)C=4C=NNC4

——

(-20℃)

With Ice Pack

≥ 2 years