CUL-4A Inhibitors
CUL-4A, a member of the cullin family of proteins, serves as a scaffold component of the E3 ubiquitin ligase complex known as CUL4-RING ligase (CRL4). CUL-4A plays a critical role in the regulation of various cellular processes, including cell cycle progression, DNA replication, DNA repair, and chromatin remodeling. As part of the CRL4 complex, CUL-4A mediates the ubiquitination and subsequent degradation of target proteins by recruiting them to the complex for ubiquitin conjugation. This process is essential for maintaining proper cellular homeostasis and integrity by regulating the levels of key regulatory proteins involved in cell cycle control, DNA damage response, and other signaling pathways.
Inhibition of CUL-4A function can have significant effects on cellular processes and signaling pathways regulated by the CRL4 complex. Several mechanisms of inhibition have been proposed, including the development of small molecule inhibitors that target specific domains or interactions essential for CUL-4A activity within the CRL4 complex. Additionally, disruption of protein-protein interactions required for the assembly or function of the CRL4 complex can impede its ability to ubiquitinate target proteins, thereby blocking their degradation and altering cellular signaling pathways. Moreover, modulation of post-translational modifications or protein stability of CUL-4A itself may also represent potential strategies for inhibiting its function and downstream effects on cellular processes. Understanding the mechanisms of CUL-4A inhibition provides insights into potential approaches for modulating cellular pathways and functions regulated by this critical E3 ubiquitin ligase complex.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $66.00 $325.00 $587.00 $1018.00 | 28 | |
ATRA inhibits CUL-4A indirectly by modulating the retinoic acid signaling pathway. It binds to retinoic acid receptors (RARs), leading to altered transcription of target genes. CUL-4A expression is downregulated as a result, impacting ubiquitin-mediated degradation pathways. | ||||||
(–)-Nutlin-3 | 675576-98-4 | sc-222086 sc-222086A | 1 mg 5 mg | $122.00 $219.00 | 2 | |
Nutlin-3 acts as an indirect CUL-4A inhibitor by disrupting the p53-MDM2 interaction. By preventing MDM2-mediated ubiquitination and degradation of p53, Nutlin-3 stabilizes p53 levels. This stabilization, in turn, influences downstream targets, including CUL-4A, affecting its ubiquitin ligase activity indirectly. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib is a proteasome inhibitor that indirectly impacts CUL-4A. By blocking the proteasomal degradation pathway, Bortezomib alters the turnover of various proteins, including those regulated by CUL-4A. This disruption leads to changes in cellular homeostasis, influencing the ubiquitin-proteasome system and, consequently, CUL-4A activity. | ||||||
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $286.00 | 1 | |
MLN4924 indirectly inhibits CUL-4A by preventing its neddylation, a crucial post-translational modification. Neddylation is essential for CUL-4A's activity as part of the E3 ubiquitin ligase complex. MLN4924 disrupts this process, resulting in the inactivation of CUL-4A and subsequent modulation of the cellular proteome. | ||||||
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, a proteasome inhibitor, indirectly affects CUL-4A by blocking the degradation of ubiquitinated proteins. This disruption in proteasomal activity leads to the accumulation of specific substrates targeted by CUL-4A, altering cellular processes regulated by CUL-4A ubiquitin ligase activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 indirectly inhibits CUL-4A by targeting the PI3K/AKT signaling pathway. As a PI3K inhibitor, it modulates downstream effectors, including CUL-4A. By disrupting the PI3K/AKT pathway, LY294002 influences the stability and activity of CUL-4A, leading to changes in substrate ubiquitination and subsequent cellular responses. | ||||||
6-Aminonicotinamide | 329-89-5 | sc-278446 sc-278446A | 1 g 5 g | $156.00 $398.00 | 3 | |
6-Aminonicotinamide indirectly inhibits CUL-4A by disrupting the NAD+ salvage pathway. This small molecule interferes with enzymes involved in NAD+ biosynthesis, impacting cellular redox homeostasis. The altered redox environment influences CUL-4A activity indirectly by modifying the post-translational regulation of substrates targeted for ubiquitination. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin indirectly inhibits CUL-4A by targeting the mTOR signaling pathway. By binding to FKBP12 and inhibiting mTORC1, Rapamycin modulates downstream effectors, including CUL-4A. This disruption in mTOR signaling leads to changes in the ubiquitin-mediated degradation of specific substrates, indirectly influencing CUL-4A activity. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $69.00 | 2 | |
Chloroquine indirectly inhibits CUL-4A by affecting autophagy. As an autophagy inhibitor, Chloroquine disrupts the lysosomal degradation pathway, leading to the accumulation of specific autophagic substrates. This altered autophagic flux influences cellular processes regulated by CUL-4A ubiquitin ligase activity in an indirect manner. | ||||||
SB-216763 | 280744-09-4 | sc-200646 sc-200646A | 1 mg 5 mg | $71.00 $202.00 | 18 | |
SB216763 indirectly inhibits CUL-4A by targeting the GSK-3β signaling pathway. As a GSK-3β inhibitor, it modulates downstream substrates, including CUL-4A. By disrupting GSK-3β-mediated phosphorylation events, SB216763 influences the stability and activity of CUL-4A, leading to changes in substrate ubiquitination and subsequent cellular responses. | ||||||