HARS2 Inhibitors
HARS2 inhibitors include a range of chemical compounds that exert their inhibitory effects through various biochemical mechanisms, affecting the functional activity of HARS2. One class of these compounds acts by compromising the process of tRNA charging, through competitive inhibition within the aminoacyl-tRNA synthetase family, ultimately reducing the efficiency of histidine attachment to tRNA, which is the primary function of HARS2. Others achieve inhibition by binding to the eukaryotic ribosomal subunit, specifically targeting the translocation or elongation steps in protein synthesis, leading to an indirect decrease in the amount of HARS2 synthesized, as the overall protein synthesis is hampered. Furthermore, some compounds chelate essential metal ions, which could compromise any metal-dependent enzymatic activity of HARS2, while others create a scarcity of cellular ATP, a necessary cofactor for the ligation action performed by HARS2, thusindirectly limiting its activity.
Additional mechanisms by which these inhibitors function include the interference with various stages of the protein synthesis machinery. Certain inhibitors mimic aminoacyl-tRNA, leading to premature termination of the growing polypeptide chain, which subsequently lowers the production of HARS2. There are also inhibitors that target the ribosomal subunit, preventing the peptidyl transferase reaction, or that freeze the ribosome's progress, thereby stalling the synthesis processes that are crucial for HARS2 production. Some function by disrupting mitochondrial protein synthesis, which could indirectly affect the mitochondrial form of HARS2. Moreover, there are inhibitors that act on the transcriptional level, inhibiting RNA polymerase II and subsequently decreasing the mRNA available for HARS2 synthesis.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Halofuginone | 55837-20-2 | sc-507290 | 100 mg | $1740.00 | ||
An inhibitor of aminoacyl-tRNA synthetase activity that specifically blocks the prolyl-tRNA synthetase. HARS2 is a homologous synthetase for histidine, and halofuginone's effect on tRNA charging efficiency would thereby reduce HARS2 activity due to competitive inhibition within the aminoacyl-tRNA synthetase class. | ||||||
Cycloheximide | 66-81-9 | sc-3508B sc-3508 sc-3508A | 100 mg 1 g 5 g | $40.00 $82.00 $256.00 | 127 | |
Binds to the eukaryotic 60S ribosomal subunit, inhibiting the translocation step in protein synthesis. Though it does not directly inhibit HARS2, it leads to reduced protein synthesis including the synthesis of HARS2, indirectly decreasing its functional presence in the cell. | ||||||
L-Mimosine | 500-44-7 | sc-201536A sc-201536B sc-201536 sc-201536C | 25 mg 100 mg 500 mg 1 g | $35.00 $86.00 $216.00 $427.00 | 8 | |
A non-protein amino acid that chelates iron and zinc ions, essential cofactors for many enzymes. Depletion of these ions can result in reduced activity of metalloenzymes, affecting HARS2 activity given it requires metal ions as cofactors. | ||||||
Oligomycin | 1404-19-9 | sc-203342 sc-203342C | 10 mg 1 g | $146.00 $12250.00 | 18 | |
An inhibitor of the mitochondrial ATP synthase (complex V), which leads to depletion of cellular ATP. Since HARS2 requires ATP for the ligation of histidine to its corresponding tRNA, oligomycin indirectly inhibits HARS2 activity by depleting the necessary ATP. | ||||||
Tetracycline | 60-54-8 | sc-205858 sc-205858A sc-205858B sc-205858C sc-205858D | 10 g 25 g 100 g 500 g 1 kg | $62.00 $92.00 $265.00 $409.00 $622.00 | 6 | |
Interferes with the binding of aminoacyl-tRNA to the mRNA-ribosome complex, thus inhibiting protein elongation. As this affects protein synthesis machinery, it would result in less HARS2 being synthesized and available for its enzymatic function. | ||||||
Puromycin | 53-79-2 | sc-205821 sc-205821A | 10 mg 25 mg | $163.00 $316.00 | 436 | |
Causes premature chain termination during translation by acting as an analog of aminoacyl-tRNA, which could reduce the functional pool of HARS2 as less is produced due to interruption of proper polypeptide synthesis. | ||||||
Chloramphenicol | 56-75-7 | sc-3594 | 25 g | $53.00 | 10 | |
Binds to the 50S subunit of the bacterial ribosome, inhibiting peptidyl transferase. In eukaryotic mitochondria, which have similar ribosomes to bacteria, chloramphenicol can inhibit mitochondrial protein synthesis and thus indirectly affect HARS2 functionality within the mitochondria. | ||||||
Diphtheria Toxin, CRM Mutant | 92092-36-9 | sc-203924 | 0.25 mg | $639.00 | 1 | |
Inhibits eukaryotic elongation factor 2 (EF-2), essential for the translocation of the ribosome along mRNA during protein synthesis. By halting protein synthesis, it indirectly leads to reduced levels of HARS2 in cells. | ||||||
Fusidic acid | 6990-06-3 | sc-215065 | 1 g | $292.00 | ||
Prevents the turnover of elongation factor G (EF-G) from the ribosome, effectively freezing the ribosome during protein synthesis and indirectly reducing the synthesis of HARS2 by stalling ribosome function. | ||||||
Anisomycin | 22862-76-6 | sc-3524 sc-3524A | 5 mg 50 mg | $97.00 $254.00 | 36 | |
Inhibits peptidyl transferase activity of the 60S ribosomal subunit in eukaryotes, leading to the inhibition of protein synthesis and, as a consequence, reducing the available amount of HARS2 for tRNA-ligation reactions. | ||||||