Clk1/2-in-3

Modify Date: 2024-01-10 11:10:34

Clk1/2-in-3 Structure
Clk1/2-in-3 structure
Common Name Clk1/2-in-3
CAS Number 1005784-60-0 Molecular Weight 375.42
Density N/A Boiling Point N/A
Molecular Formula C21H21N5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Clk1/2-in-3


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].

 Names

Name CLK1/2-IN-3

 Clk1/2-in-3 Biological Activity

Description 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].
Related Catalog
Target

CLK1:1.1 nM (IC50)

CLK2:2.1 nM (IC50)

SRPK1:130 nM (IC50)

SRPK2:260 nM (IC50)

SRPK3:260 nM (IC50)

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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C21H21N5O2
Molecular Weight 375.42