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CLK1/2-IN-3

Catalog No. T23897   CAS 1005784-60-0
Synonyms: CLK1/2 inhibitor 3, CLK1/2-inhibitor-3, CLK1/2 IN 3, CLK1/2IN3

CLK1/2-IN-3 (Cpd-3) is a potent and selective CLK1 and CLK2 inhibitor with antiproliferative activity and inhibits the activities of CLK1, CLK2, SRPK1, SRPK2, and SRPK3.CLK1/2-IN-3 induces nuclear speckle enlargement, which induces S6K pre-mRNA-selective splicing and subsequent inhibition of cell growth of multiple cancer cell types. cancer cell types cell growth.

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CLK1/2-IN-3 Chemical Structure
CLK1/2-IN-3, CAS 1005784-60-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 350.00
5 mg In stock $ 970.00
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Purity: 98.71%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CLK1/2-IN-3 (Cpd-3) is a potent and selective CLK1 and CLK2 inhibitor with antiproliferative activity and inhibits the activities of CLK1, CLK2, SRPK1, SRPK2, and SRPK3.CLK1/2-IN-3 induces nuclear speckle enlargement, which induces S6K pre-mRNA-selective splicing and subsequent inhibition of cell growth of multiple cancer cell types. cancer cell types cell growth.
Targets&IC50 SRPK1:130 nM, SRPK3:260 nM, SRPK2:260 nM, CLK2:2.1 nM, CLK1:1.1 nM
In vitro Exposure to CLK1/2-IN-3 (compound 3) at concentrations of 1.1-3.3 μM for 72 hours increases the expression of S6K mRNAs in MDA-MB-468 cells[1].
Significant reduction in the levels of endogenous phosphorylated SR proteins is observed with CLK1/2-IN-3 (5 μM)[1].Anti-proliferative activity is demonstrated by CLK1/2-IN-3 (1-10 μM) 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].
Synonyms CLK1/2 inhibitor 3, CLK1/2-inhibitor-3, CLK1/2 IN 3, CLK1/2IN3
Molecular Weight 375.42
Formula C21H21N5O2
CAS No. 1005784-60-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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. 2. Jain P, Karthikeyan C, Moorthy NS, Waiker DK, Jain AK, Trivedi P. Human CDC2-like kinase 1 (CLK1): a novel target for Alzheimer's disease. Curr Drug Targets. 2014 May;15(5):539-50. Review. PubMed PMID: 24568585. 3. Montes-Grajales D, Olivero-Verbel J. Computer-aided identification of novel protein targets of bisphenol A. Toxicol Lett. 2013 Oct 9;222(3):312-20. doi: 10.1016/j.toxlet.2013.08.010. Epub 2013 Aug 20. PubMed PMID: 23973438. 4. Wong R, Balachandran A, Mao AY, Dobson W, Gray-Owen S, Cochrane A. Differential effect of CLK SR Kinases on HIV-1 gene expression: potential novel targets for therapy. Retrovirology. 2011 Jun 17;8:47. doi: 10.1186/1742-4690-8-47. PubMed PMID: 21682887; PubMed Central PMCID: PMC3148977.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library

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Keywords

CLK1/2-IN-3 1005784-60-0 Cell Cycle/Checkpoint CDK CLK1/2 inhibitor 3 CLK1/2-inhibitor-3 CLK1/2 IN 3 CLK1/2IN3 CLK-1/2-IN-3 inhibitor inhibit

 

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