KCMF1 Inhibitors
Chemical inhibitors of KCMF1 include a variety of compounds that target the proteasome pathway, in which KCMF1 plays a role through its ubiquitin ligase activity. Staurosporine acts upstream of KCMF1, inhibiting protein kinases that regulate the phosphorylation state of various proteins, including possibly those interacting with KCMF1. This inhibition can decrease the functional activity of KCMF1 by preventing the necessary post-translational modifications that activate the protein or its substrates. MG-132 and Lactacystin, both proteasome inhibitors, can lead to the accumulation of ubiquitinated proteins by blocking their degradation. This build-up can create a feedback loop that hinders KCMF1's ability to ubiquitinate further substrates, as the pathway becomes saturated with undegraded proteins.
Similarly, Bortezomib, Withaferin A, and Epoxomicin, which selectively target various activities of the proteasome, can indirectly inhibit KCMF1 by preventing the proteolytic breakdown of its ubiquitinated targets. This results in a bottleneck effect where the continuous tagging of proteins for degradation by KCMF1 is rendered ineffective due to the inhibited proteolytic capacity. Carfilzomib's irreversible binding to the proteasome exacerbates this effect, leading to a more sustained inhibition of KCMF1's functional role in protein turnover. Oprozomib, Marizomib, and Ixazomib work similarly by obstructing the proteasomal degradation pathway, which is essential for the culmination of KCMF1's role in regulating protein levels within the cell. Velcade, or Bortezomib under a different name, is noteworthy for its precise action on the proteasome, further substantiating the approach of using proteasome inhibitors to indirectly affect the functional activity of KCMF1 by halting the degradation process of ubiquitinated proteins, thereby stalling the protein turnover cycle that KCMF1 is designed to facilitate.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine inhibits protein kinases, and since KCMF1 has ubiquitin ligase activity, inhibition of upstream kinases that regulate KCMF1's phosphorylation state could inhibit its function. | ||||||
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 is a proteasome inhibitor. KCMF1 is suggested to have a role in ubiquitination, which targets proteins for degradation via the proteasome. Inhibiting the proteasome could lead to the accumulation of ubiquitinated proteins, indirectly inhibiting KCMF1's ability to mediate further ubiquitination. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $188.00 $575.00 | 60 | |
Lactacystin is another proteasome inhibitor, and similar to MG-132, it would inhibit the degradation pathway of proteins ubiquitinated by KCMF1, potentially leading to an inhibition of KCMF1's functional role in protein turnover. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib specifically targets the 26S proteasome complex. By inhibiting this complex, the degradation of ubiquitinated proteins is prevented, which could inhibit KCMF1's ability to tag proteins for degradation. | ||||||
Withaferin A | 5119-48-2 | sc-200381 sc-200381A sc-200381B sc-200381C | 1 mg 10 mg 100 mg 1 g | $130.00 $583.00 $4172.00 $20506.00 | 20 | |
Withaferin A is known to inhibit the proteasomal pathway. By doing so, it could indirectly inhibit KCMF1 by preventing the degradation of proteins it has ubiquitinated, thus interfering with its normal function. | ||||||
Epoxomicin | 134381-21-8 | sc-201298C sc-201298 sc-201298A sc-201298B | 50 µg 100 µg 250 µg 500 µg | $137.00 $219.00 $449.00 $506.00 | 19 | |
Epoxomicin is a selective proteasome inhibitor. By inhibiting the proteasome, KCMF1's function in ubiquitin-dependent protein degradation is indirectly inhibited as the downstream effect of ubiquitination is blocked. | ||||||
Carfilzomib | 868540-17-4 | sc-396755 | 5 mg | $41.00 | ||
Carfilzomib irreversibly binds to and inhibits the proteasome. This prevents the degradation of ubiquitinated proteins and indirectly inhibits the functional activity of KCMF1 in the ubiquitin-proteasome pathway. | ||||||
Oprozomib | 935888-69-0 | sc-477447 | 2.5 mg | $280.00 | ||
Oprozomib is an oral proteasome inhibitor. It would inhibit the function of KCMF1 by blocking the degradation of proteins that KCMF1 has tagged for degradation, thereby inhibiting its role in proteostasis. | ||||||
Ixazomib | 1072833-77-2 | sc-489103 sc-489103A | 10 mg 50 mg | $311.00 $719.00 | ||
Ixazomib is a small molecule proteasome inhibitor. By inhibiting the proteasome, it would prevent the degradation of proteins ubiquitinated by KCMF1, thus indirectly inhibiting KCMF1's ubiquitin ligase activity. | ||||||