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].

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].

375.42

C₂₁H₂₁N₅O₂

1005784-60-0

Room temperature in continental US; may vary elsewhere.

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