1005784-60-0

1005784-60-0 structure

Name: Clk1/2-in-3
Chemical Name: CLK1/2-IN-3
CAS Number: 1005784-60-0
Molecular Formula: C₂₁H₂₁N₅O₂
Molecular Weight: 375.42
Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
Create Date: 2022-08-21 11:20:30
Modify Date: 2024-01-10 11:10:34
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].

Name	CLK1/2-IN-3

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	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> SRPK Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
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.

Molecular Formula	C₂₁H₂₁N₅O₂
Molecular Weight	375.42