CUL-3 Inhibitors
CUL-3 inhibitors belong to a distinct chemical class that plays a pivotal role in regulating cellular processes through the disruption of Cullin-3 (CUL-3)-based E3 ubiquitin ligase complexes. The CUL-3 protein serves as a critical component in the ubiquitin-proteasome system (UPS), an intricate cellular machinery responsible for the targeted degradation of specific proteins. CUL-3, when bound to its associated BTB (Broad Complex, Tramtrack, and Bric-a-Brac) domain-containing substrate adaptors, recruits target proteins for ubiquitination, marking them for degradation by the proteasome. CUL-3 inhibitors act as small molecules or compounds that disrupt the assembly or activity of CUL-3 E3 ligase complexes, thereby altering the fate of their substrate proteins.
Structurally diverse, CUL-3 inhibitors can exert their inhibitory effects through multiple mechanisms. Some compounds directly bind to CUL-3 or its substrate adaptors, interfering with their interaction and preventing the formation of the functional E3 ligase complex. Others may impact downstream ubiquitination processes by affecting the recruitment of ubiquitin-conjugating enzymes or proteasomal degradation itself. These inhibitors have garnered significant interest in the realm of basic research, where they serve as valuable tools for dissecting the intricate roles of specific target proteins within cellular pathways. Furthermore, by modulating the stability of specific proteins, CUL-3 inhibitors have the ability to offer insights into the molecular underpinnings of various cellular processes, shedding light on the intricacies of protein regulation and degradation in both normal and pathological contexts. Thus, CUL-3 inhibitors represent a crucial class of compounds in the toolkit of molecular biologists and cell biologists for their ability to manipulate and investigate protein dynamics in a controlled and precise manner.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
MLN 4924 | 905579-51-3 | sc-484814 | 1 mg | $280.00 | 1 | |
MLN4924 inhibits CUL-3 neddylation by targeting NEDD8-activating enzyme (NAE), preventing the conjugation of NEDD8 to CUL-3. This disrupts CUL-3's ability to function as part of the CRL E3 ubiquitin ligase complex, leading to the stabilization of its substrate proteins. | ||||||
Auranofin | 34031-32-8 | sc-202476 sc-202476A sc-202476B | 25 mg 100 mg 2 g | $150.00 $210.00 $1899.00 | 39 | |
Auranofin indirectly inhibits CUL-3 by modulating the cellular redox state and affecting the stability of proteins regulated by CUL-3-containing CRL complexes. It disrupts the function of CUL-3 E3 ligases by altering the redox environment within cells. | ||||||
Piperlongumine | 20069-09-4 | sc-364128 | 10 mg | $107.00 | ||
Piperlongumine inhibits CUL-3-dependent ubiquitination by interfering with the assembly of the CRL complex. It hinders the binding of substrate proteins to the CUL-3 ligase, thereby preventing their ubiquitination and degradation. | ||||||
Thalidomide | 50-35-1 | sc-201445 sc-201445A | 100 mg 500 mg | $109.00 $350.00 | 8 | |
Thalidomide indirectly targets CUL-3 by modulating the activity of CUL-4 E3 ligases, which share similarities with CUL-3-containing complexes. It disrupts the ubiquitination and degradation of proteins regulated by CUL-3-like E3 ligases. | ||||||
MLN7243 | 1450833-55-2 | sc-507338 | 5 mg | $340.00 | ||
MLN7243 inhibits CUL-3 neddylation similar to MLN4924, preventing the activation of CUL-3 by NEDD8. This results in the stabilization of CUL-3 substrate proteins as they are not ubiquitinated and targeted for degradation. | ||||||
Nutlin-3 | 548472-68-0 | sc-45061 sc-45061A sc-45061B | 1 mg 5 mg 25 mg | $56.00 $212.00 $764.00 | 24 | |
Nutlin-3 indirectly affects CUL-3 activity by inhibiting the interaction between p53 and MDM2, leading to the stabilization of p53. This stabilization can result in altered cellular processes regulated by CUL-3, as p53 is one of its substrates. | ||||||
Flavopiridol | 146426-40-6 | sc-202157 sc-202157A | 5 mg 25 mg | $78.00 $254.00 | 41 | |
Flavopiridol inhibits CUL-3-dependent ubiquitination by interfering with the assembly of the CRL complex. It disrupts the binding of substrate proteins to the CUL-3 ligase, preventing their ubiquitination and subsequent degradation. | ||||||
Spautin-1 | 1262888-28-7 | sc-507306 | 10 mg | $165.00 | ||
Spautin-1 disrupts the CUL-3-dependent autophagy pathway by inhibiting the interaction between CUL-3 and BECN1, a key regulator of autophagy. This leads to the accumulation of autophagic substrates and the inhibition of autophagy. | ||||||