A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore was written by Shi, Yihui;Park, Jaehyeon;Lagisetti, Chandraiah;Zhou, Wei;Sambucetti, Lidia C.;Webb, Thomas R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Recommanded Product: 203436-45-7 This article mentions the following:
The splicing of pre-mRNA is a critical process in normal cells and is deregulated in cancer. Compounds that modulate this process have recently been shown to target a specific vulnerability in tumors. We have developed a novel cell-based assay that specifically activates luciferase in cells exposed to SF3B1 targeted compounds, such as sudemycin D6. This assay was used to screen a combined collection of approved drugs and bioactive compounds This screening approach identified several active hits, the most potent of which were CGP-74514A and aminopurvalanol A, both have been reported to be cyclin-dependent kinases (CDKs) inhibitors. We found that these compounds, and their analogs, show significant cdc2-like kinase (CLK) inhibition and clear structure-activity relationships (SAR) at CLKs. We prepared a set of analogs and were able to ‘dial out’ the CDK activity and simultaneously developed CLK inhibitors with low nanomolar activity. Thus, we have demonstrated the utility of our exon-skipping assay and identified new mols. that exhibit potency and selectivity for CLK, as well as some structurally related dual CLK/CDK inhibitors. In the experiment, the researchers used many compounds, for example, 2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7Recommanded Product: 203436-45-7).
2,6-Dichloro-9-isopropyl-9H-purine (cas: 203436-45-7) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Recommanded Product: 203436-45-7
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics