DPH2 inhibitors are a class of compounds that target and inhibit the activity of the DPH2 enzyme, which plays a critical role in the biosynthesis of diphthamide, a unique post-translationally modified histidine residue found in elongation factor 2 (eEF2). Diphthamide is essential for the proper functioning of eEF2, a key protein involved in the process of protein synthesis by facilitating the translocation of ribosomes during translation. The DPH2 enzyme catalyzes one of the early steps in the multi-step pathway responsible for the biosynthesis of diphthamide, specifically converting a precursor histidine residue on eEF2 into diphthine, a key intermediate. Inhibition of DPH2 disrupts this biosynthetic pathway, potentially affecting the modification of eEF2 and thus influencing protein synthesis.
The mode of action of DPH2 inhibitors typically involves interfering with the enzyme's active site or blocking the substrates required for the diphthamide biosynthesis process. By inhibiting DPH2, these compounds can lead to a reduction in diphthamide-modified eEF2, thereby altering the efficiency of ribosomal translocation and overall protein synthesis. Since the modification of eEF2 by diphthamide is highly conserved and crucial for its function, DPH2 inhibitors can have broad implications on cellular processes that rely on effective protein synthesis. This chemical class provides important tools for studying the regulation of protein translation and the role of post-translational modifications in protein function, particularly in understanding how specific enzymatic pathways contribute to the modification and regulation of key cellular machinery.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Trichostatin A | 58880-19-6 | sc-3511 sc-3511A sc-3511B sc-3511C sc-3511D | 1 mg 5 mg 10 mg 25 mg 50 mg | $152.00 $479.00 $632.00 $1223.00 $2132.00 | 33 | |
Trichostatin A may inhibit the transcription of DPH2 by increasing acetylation of histones and opening chromatin structure, rendering the DPH2 gene less accessible to transcriptional machinery. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine could lead to the downregulation of DPH2 by promoting DNA demethylation, which may activate transcriptional repressors or silence activators of DPH2 expression. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin (Sirolimus) might decrease DPH2 expression by inhibiting the mTOR pathway, which is responsible for the regulation of protein synthesis, including the synthesis of proteins that control the expression of DPH2. | ||||||
Actinomycin D | 50-76-0 | sc-200906 sc-200906A sc-200906B sc-200906C sc-200906D | 5 mg 25 mg 100 mg 1 g 10 g | $74.00 $243.00 $731.00 $2572.00 $21848.00 | 53 | |
Actinomycin D could directly inhibit the transcription of DPH2 by binding to its DNA sequence, specifically intercalating between guanine-cytosine base pairs, blocking RNA polymerase movement. | ||||||
Cycloheximide | 66-81-9 | sc-3508B sc-3508 sc-3508A | 100 mg 1 g 5 g | $41.00 $84.00 $275.00 | 127 | |
Cycloheximide may reduce DPH2 protein levels indirectly by halting global protein synthesis, including the translation of DPH2 mRNA into the DPH2 enzyme. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $69.00 | 2 | |
Chloroquine could decrease the stability of DPH2 mRNA by disrupting lysosomal degradation pathways and autophagy processes, which may lead to the degradation of mRNA transcripts, including those of DPH2. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $60.00 $265.00 $1000.00 | 163 | |
MG-132 may lead to the accumulation of ubiquitinated proteins that can sequester transcription factors or other proteins involved in the regulation of DPH2, thereby reducing its expression. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY 294002 could downregulate DPH2 expression by inhibiting PI3K, leading to a suppression of the downstream AKT signaling pathway and potentially reducing the transcriptional activity of genes like DPH2. | ||||||
SN 38 | 86639-52-3 | sc-203697 sc-203697A sc-203697B | 10 mg 50 mg 500 mg | $119.00 $342.00 $883.00 | 19 | |
SN 38 may decrease the levels of DPH2 by inhibiting topoisomerase I, causing DNA damage and activating cellular responses that shut down non-essential gene expression, including DPH2. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $133.00 $275.00 | 37 | |
Suberoylanilide Hydroxamic Acid (Vorinostat) could downregulate DPH2 by inhibiting histone deacetylases, causing an accumulation of acetylated histones, which may repress transcription of specific genes, potentially including DPH2. | ||||||