KLHL21 Inhibitors
KLHL21 Inhibitors encompass a range of chemical compounds that target the ubiquitination pathway, which is critical for protein turnover and regulation. Proteasome inhibitors such as MG-132 and Bortezomib impede the degradation of ubiquitinated proteins, resulting in the accumulation of KLHL21's substrates and a consequential indirect inhibition of KLHL21's role in the ubiquitin-proteasome system. Similarly, MLN 4924 (Pevonedistat) targets upstream processes by inhibiting the NEDD8-activating enzyme, essential for the activation of Cullin 3, a core component of the E3 ubiquitin ligase complex involving KLHL21. Curcumin and Chloroquine further contribute to the inhibition of KLHL21 by disrupting protein-protein interactions within the E3 ligase complex and by impeding autophagic degradation of ubiquitinated proteins, respectively, leading to a decrease in KLHL21's functional activity.
In addition to these, compounds like Thalidomide, Lenalidomide, and Pomalidomide indirectly inhibit KLHL21 by potentially affecting the assembly and function of E3 ubiquitin ligase complexes through their interaction with cereblon, a substrate receptor for a related E3 ligase. The ubiquitination process is also targeted by MLN7243, an E1 enzyme inhibitor, along with PYR-41, which by the same mechanism, diminishes KLHL21's ability to ubiquitinate substrates. Auranofin, with its impact on redox regulation, may alter the functional state of proteins within the E3 ligase complex, indirectly inhibiting KLHL21. Finally, MLN8237 (Alisertib), an inhibitor of Aurora kinase A, can also attenuate KLHL21 activity by modifying the phosphorylation status of potential KLHL21 substrates, highlighting the intricate interplay between phosphorylation and ubiquitination pathways in regulating protein stability. Together, these KLHL21 inhibitors collectively impede the ubiquitin-proteasome system by various mechanisms, emphasizing the complex regulation of protein degradation processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $56.00 $260.00 $980.00 | 163 | |
MG-132 is a proteasome inhibitor that prevents the degradation of ubiquitinated proteins. Since KLHL21 is an adaptor for the Cullin 3-based E3 ubiquitin ligase complex, which tags proteins for proteasomal degradation, MG-132 indirectly inhibits KLHL21 function by blocking the proteasome, leading to the accumulation of its substrates. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $132.00 $1064.00 | 115 | |
Bortezomib is a proteasome inhibitor that functions similarly to MG132. By preventing the degradation of ubiquitinated proteins, Bortezomib indirectly diminishes the function of KLHL21 by causing the substrates it targets for degradation to accumulate. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $280.00 | 1 | |
MLN 4924 is an inhibitor of NEDD8-activating enzyme (NAE), which is essential for cullin-RING ligase function. By inhibiting NAE, MLN 4924 prevents the neddylation of Cullin 3, thereby indirectly inhibiting KLHL21 activity by blocking the formation of the active E3 ubiquitin ligase complex. | ||||||
Thalidomide | 50-35-1 | sc-201445 sc-201445A | 100 mg 500 mg | $109.00 $350.00 | 8 | |
Thalidomide and its derivatives bind to the protein cereblon, a substrate receptor for the Cullin 4 E3 ubiquitin ligase complex. Its binding can affect the assembly and function of related cullin-RING ligase complexes, potentially diminishing KLHL21 activity indirectly by disrupting similar E3 ligase complexes. | ||||||
Lenalidomide | 191732-72-6 | sc-218656 sc-218656A sc-218656B | 10 mg 100 mg 1 g | $49.00 $367.00 $2030.00 | 18 | |
Lenalidomide is a derivative of thalidomide that binds to cereblon. This interaction may lead to a decrease in KLHL21 functional activity by altering the assembly of Cullin 3-containing E3 ubiquitin ligase complexes through competitive inhibition or allosteric effects. | ||||||
Pomalidomide | 19171-19-8 | sc-364593 sc-364593A sc-364593B sc-364593C sc-364593D sc-364593E | 5 mg 10 mg 50 mg 100 mg 500 mg 1 g | $98.00 $140.00 $306.00 $459.00 $1224.00 $1958.00 | 1 | |
Pomalidomide is a thalidomide derivative with similar properties. Its binding to cereblon could indirectly inhibit KLHL21 by affecting the formation or activity of Cullin 3-based E3 ubiquitin ligase complexes, to which KLHL21 contributes. | ||||||
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin is known to interfere with several signaling pathways and may indirectly inhibit KLHL21 by modifying the protein-protein interactions within the E3 ubiquitin ligase complex, thus preventing KLHL21 from effectively targeting its substrates for ubiquitination. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $68.00 | 2 | |
Chloroquine is an autophagy inhibitor that can lead to the accumulation of ubiquitinated proteins. Since KLHL21 is part of the ubiquitination machinery, chloroquine indirectly inhibits KLHL21 function by reducing the degradation of ubiquitinated proteins via autophagy, causing a backlog of substrates. | ||||||
MLN7243 | 1450833-55-2 | sc-507338 | 5 mg | $340.00 | ||
MLN7243 is an inhibitor of the ubiquitin-activating enzyme E1. By inhibiting E1, MLN7243 indirectly diminishes KLHL21 activity by reducing the overall ubiquitination process, including the ubiquitination mediated by the Cullin 3-KLHL21 E3 ligase complex. | ||||||
MLN8237 | 1028486-01-2 | sc-394162 | 5 mg | $220.00 | ||
MLN8237 is an Aurora kinase A inhibitor. Although it primarily targets mitotic kinases, it can indirectly affect KLHL21 by altering the phosphorylation state of proteins that may be substrates for KLHL21, leading to changes in their ubiquitination and degradation. | ||||||