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E3 ligase ligands bind ubiquitin ligases such as cereblon and von Hippel-Lindau (VHL) in degrader design. In a degrader, they anchor the ligase end of the molecule. E3 ubiquitin ligases transfer ubiquitin to substrate proteins and mark them for degradation by the proteasome. Thalidomide and its analogs bind cereblon (CRBN), a substrate receptor of a cullin-based E3 ligase complex identified as their direct target in 2010. The category includes cereblon ligands such as thalidomide fluoride and TD-106, and VHL ligands such as VL285 and VH032-cyclopropane-F. These ligands are used to build proteolysis-targeting chimeras (PROTACs) and to study how ligases are recruited to new substrates.
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCFFbxo3 catalyzed Fbxl2 ubiquitination.
Synonyms: VHL ligand 6
VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
Cereblon inhibitor 2 is an effective inhibitor of the Cereblon protein, primarily targeting its role in regulating substrate degradation through the CRL4 E3 ubiquitin ligase complex. This compound exhibits significant biological activity in inhibiting cancer cell proliferation and enhancing apoptosis, making it a valuable tool in solid tumor research, particularly in breast cancer studies. Its application may facilitate advancements in understanding the molecular mechanisms underlying tumor biology and therapeutic resistance.
VHL-IN-1 is an inhibitor of the von Hippel-Lindau (VHL) ubiquitin E3 ligase with a dissociation constant (Kd) of 37 nM. It effectively stabilizes and enhances the transcriptional activity of HIF-1α, which plays a crucial role in cellular responses to hypoxia. VHL-IN-1 is potentially valuable in research applications aimed at exploring HIF-1α regulation and the development of proteolytically targeted chimeras (PROTACs) for targeted protein degradation.
Synonyms: Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl
PPACK dihydrochloride is a potent and selective irreversible inhibitor of thrombin. It serves as an alternative anticoagulant to lithium heparin for blood gas and electrolyte analyses in whole blood. Additionally, PPACK dihydrochloride inhibits plasminogen activator (rt-PA), preventing its binding to plasma protease inhibitors. This compound also reduces plasmin-induced endothelial permeability and morphological changes in bovine aortic endothelial cell monolayers, making it suitable for investigations in thrombosis-related research.
VH032 is a potent ligand for the von Hippel-Lindau (VHL) protein, acting primarily by inhibiting the interaction between VHL and hypoxia-inducible factor 1-alpha (HIF-1α). Its high affinity and specificity make VH032 an essential tool for research applications involving targeted protein degradation through PROTAC technology. This compound facilitates the study of VHL-mediated pathways and the regulation of hypoxic responses in various biological contexts.
MEL24 is an inhibitor of the Mdm2 E3 ligase, which plays a critical role in regulating p53 protein levels. This compound significantly reduces cell survival and enhances sensitivity to DNA-damaging agents in a p53-dependent manner. MEL24 is primarily utilized in antitumor research, contributing to studies aimed at understanding and overcoming resistance in cancer therapies.
SJ1008066 is an inhibitor of the MAGE-A11 protein, demonstrating an IC50 of 0.13 μM. It specifically binds to the MAGE homology domain (MHD), effectively disrupting the interaction between MAGE-A11 and PCF11. This mechanism presents valuable opportunities for research into cancer biology and therapeutic strategies targeting MAGE-A11 associated pathways.
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MEL23 is an MDM2 E3 ligase inhibitor that specifically targets the E3 ligase activity of the MDM2-MDMX complex. This compound effectively inhibits the ubiquitination of MDM2 and p53, leading to decreased viability in cells expressing wild-type p53. Additionally, MEL23 stabilizes MDM2 through a mechanism that does not involve p53 transcription, making it a valuable tool for research into cancer biology and therapeutic strategies targeting the p53 pathway.
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E3 ligase Ligand 66 is an E3 ligase ligand designed to specifically recruit inhibitor of apoptosis (IAP) proteins. This compound facilitates targeted protein degradation through the formation of PROTACs when conjugated with ligands such as SARS-CoV-2 Mpro ligand 1, enabling researchers to manipulate protein levels in cellular systems. Its applications extend to investigations in degradation pathways and therapeutic strategies against diseases, including viral infections.
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