1005784-60-0

CLK1/2-IN-3 is a selective CLK1 and CLK2 inhibitor.

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].

CLK1: 1.1 nM (IC₅₀); CLK2: 2.1 nM (IC₅₀); SRPK1: 130 nM (IC₅₀); SRPK2: 260 nM (IC₅₀); SRPK3: 260 nM (IC₅₀)

[1] Araki S, et al. Inhibitors of CLK protein kinases suppress cell growth and induce apoptosis by modulating pre-mRNA splicing. PLoS One. 2015;10(1):e0116929. Published 2015 Jan 12. DOI:10.1371/journal.pone.0116929