HIF PHD3 Inhibitors
HIF PHD3 inhibitors encompass a range of chemicals that indirectly affect the activity of the enzyme, primarily through the modulation of HIF stability and activity. These inhibitors act upon the oxygen-sensing pathway that is central to the cellular response to hypoxia. The primary mechanism of action for these inhibitors involves the competitive inhibition of the HIF PHD3 active site, deprivation of essential cofactors like iron, or the disruption of HIF's interaction with transcriptional coactivators. Compounds such as DMOG, IOX2, and various PHD inhibitors mimic hypoxic conditions by hindering the hydroxylation of HIF, thereby stabilizing HIF-1α and promoting the transcription of hypoxia-inducible genes.
The use of these inhibitors increase the transcriptional activity of HIF-1α, leading to an augmented cellular response to hypoxia. This may result in the upregulation of a suite of genes involved in erythropoiesis, angiogenesis, and metabolism. In the case of MAGE-A12, while it is not a direct substrate of PHD3, the stabilization of HIF influence the expression of genes within the same pathways or networks as MAGE-A12, altering its expression or function. The theoretical use of these inhibitors to modulate MAGE-A12 activity would require a nuanced understanding of the cellular context and the interplay between HIF signaling and the expression of cancer/testis antigens.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Dimethyloxaloylglycine (DMOG) | 89464-63-1 | sc-200755 sc-200755A sc-200755B sc-200755C | 10 mg 50 mg 100 mg 500 mg | $84.00 $301.00 $374.00 $779.00 | 25 | |
DMOG is a cell-permeable analog of 2-oxoglutarate that competitively inhibits HIF PHD enzymes, potentially including PHD3, leading to the stabilization of HIF proteins under normoxic conditions. | ||||||
IOX2 | 931398-72-0 | sc-482692 sc-482692A sc-482692B | 5 mg 25 mg 100 mg | $131.00 $566.00 $1613.00 | ||
IOX2 is a potent inhibitor of HIF PHD enzymes that can theoretically reduce PHD3 activity, resulting in the accumulation of HIF-1α and enhanced transcription of hypoxia-responsive genes. | ||||||
N-[(4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine-d3 | 808118-40-3 unlabeled | sc-488006 | 10 mg | $12000.00 | ||
N-[(4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine-d3 is a PHD inhibitor that could indirectly inhibit PHD3, thereby increasing HIF activity and stimulating erythropoiesis, especially under hypoxic conditions. | ||||||
BAY 85-3934 | 1154028-82-6 | sc-507384 | 5 mg | $205.00 | ||
Molidustat is a PHD inhibitor designed to stabilize HIF-1α by potentially inhibiting PHD3, thereby influencing the body’s production of erythropoietin (EPO). | ||||||
L-Mimosine | 500-44-7 | sc-201536A sc-201536B sc-201536 sc-201536C | 25 mg 100 mg 500 mg 1 g | $36.00 $88.00 $220.00 $436.00 | 8 | |
L-Mimosine is an iron chelator and amino acid analog that can inhibit HIF PHD enzymes by depriving them of necessary cofactors like iron, possibly affecting PHD3. | ||||||
Deferoxamine mesylate | 138-14-7 | sc-203331 sc-203331A sc-203331B sc-203331C sc-203331D | 1 g 5 g 10 g 50 g 100 g | $255.00 $1060.00 $2923.00 $4392.00 $8333.00 | 19 | |
Deferoxamine mesylate is another iron chelator that sequesters iron, a cofactor essential for HIF PHD enzyme activity, and could thus indirectly inhibit PHD3. | ||||||
Cobalt(II) chloride | 7646-79-9 | sc-252623 sc-252623A | 5 g 100 g | $64.00 $176.00 | 7 | |
Cobalt(II) chloride mimics hypoxia by inhibiting HIF PHD enzymes, including potentially PHD3, resulting in the upregulation of HIF and its target genes. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol is a quinone methide triterpenoid that has been shown to inhibit HIF-1α degradation and could potentially inhibit PHD3 indirectly by modulating proteasomal degradation pathways. | ||||||
Chetomin | 1403-36-7 | sc-202535 sc-202535A | 1 mg 5 mg | $186.00 $674.00 | 10 | |
Chetomin disrupts the interaction between HIF-1α and p300/CBP, potentially affecting HIF PHD3 indirectly by altering HIF-1α transcriptional activity. | ||||||