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| TCI Life Science News June 2021 | ||||
| At TCI, we support discovery in life sciences through our knowledge and expertise in organic small molecules. In this issue we focus on our building blocks for synthesis of proteolysis targeting compounds, anti-tuberculosis research reagents, HMG-CoA reductase inhibitors, and chemiluminescence reagents. We also have thousands of other useful compounds available only at TCI for your research and development. | ||||
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Building Blocks for Synthesis of Proteolysis Targeting CompoundsIn recent years, research in medicinal chemistry has increased the investigation in the use of the ubiquitin-proteasome system (UPS) to combat diseases. As a result, a variety of chimera compounds have been synthesized consisting of a tag that can bind to ubiquitin ligase, a linker and another ligand that can bind to disease related proteins. This enables us to bring the disease related protein in proximity to an activated UPS to eliminate the protein. Measuring the activity of these compounds has shown that the length of the linker is an important factor in triggering ubiquitination. TCI now offers hetero-bifunctional linkers with a variety of lengths. | ||||
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Anti-tuberculosis Research Reagents2-trans-Dodecanoyl-CoA [D5661] acts on enoyl-ACP reductase (InhA) as one of 2-trans-enoyl-ACP, a substrate for InhA in the synthesis pathway of fatty acids, which constitute the cell wall of Mycobacterium tuberculosis. Therefore, it is reported that InhA inhibiiton assay by measuring InhA's reducing activity of 2-trans-Dodecanoyl-CoA can be applied for the screening of anti-tuberculosis agent candidates. | ||||
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HMG-CoA Reductase Inhibitors (Statins)The statins inhibit the action of HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase that catalyzes the rate-limiting step in cholesterol biosynthesis, resulting in the reduction of low-density-lipoprotein (LDL) and total cholesterol levels. Especially in statins, atorvastatin [A2476] is a most potent inhibitor due to its a long half-life and metabolites which also play a role as an HMG-CoA reductase inhibitor. Lovastatin [L0214], mevastatin [M2275] and simvastatin [S0509] are pro-drug ingredients that are activated by in vivo hydrolysis of the lactone ring. Many statins are metabolized by cytochrome P450 3A4 (CYP3A4) while fluvastatin [F0820] is metabolized by CYP2C9. | ||||
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Chemiluminescence ReagentsChemiluminescence is the phenomenon of energy released as light when the excited state of molecules by oxidation returns to the ground state. Organic substances which exhibit chemiluminescene are Cypridina luciferin analog, firefly luciferin, oxalate, luminol and acridinium, etc. TCI also offers chemiluminescence enhancers for chemiluminescent enzyme immunoassays. | ||||
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