Home Ubiquitin E3 Ligase

E3 Ligase Inhibitors/Modulators

Other Ubiquitin Related Inhibitors

E1 Activating DUB E2 conjugating p97 SUMO TRAF

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S8760 Iberdomide (CC-220) Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities.
Cell Rep Med, 2025, S2666-3791(25)00102-8
J Med Virol, 2025, 97(8):e70537
Cancer Res, 2025, 10.1158/0008-5472.CAN-24-1136
S1061 Nutlin-3 Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.
Cancer Discov, 2025, 15(1):69-82
iScience, 2025, 28(6):112635
Biomed Rep, 2025, 22(4):65
Verified customer review of Nutlin-3
S8652 Skp2 inhibitor C1 (SKPin C1) Skp2 inhibitor C1 (SKPin C1) is a specific and selective small-molecule inhibitor of Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
British Journal of Cancer, September 29 2022, 2072-2085
OncoTargets and Therapy, May 30 2019, 4297-4308
Journal of Clinical Investigation, December 15 2022, e153943
S9605 Apcin Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.
bioRxiv, May 2, 2025, 2025.04.28.651139
Experimental Hematology & Oncology, March 7, 2023, 28
Cellular & Molecular Biology Letters, March 2025, 29
S7892 Avadomide (CC-122) Avadomide (CC-122) is a new chemical entity termed pleiotropic pathway modifier and a novel agent for Diffuse large B-cell lymphoma (DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.
Molecular Therapy - Oncolytics, June 23, 2020, 215-225
bioRxiv, June 08, 2025, nan
Blood Advances, July 23, 2019, 2105-2117
S5315 PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.
bioRxiv, May 09, 2023, 2023.05.08.539886
Nat Commun, 2023, 10.1038/s41467-023-42930-y
British Journal of Cancer, 2023, 232-244
S0095 VL285 VL285 is a potent VHL ligand that degrades HaloTag7 fusion proteins. Cotreatment with excess this compound, the core VHL ligand from which HaloPROTAC3 is derived, is able to significantly reduce HaloPROTAC3 mediated activity to 50% degradation.
bioRxiv, 2025, 2024.03.24.586276
Cell Death & Differentiation, 2024, 592-604
Int J Mol Sci, 2024, 25(16)8984
S9724 SZL P1-41 SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells and cancer stem cells. This compound causes higher apoptosis rates in cancer cells.
Cell Death Discovery, October 02, 2023, 364
Cell Biology and Toxicology, 2025, 135
J Immunother Cancer, 2024, 12(12)e009444
S8449 VH298 VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. This compound blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. It can be used in PROTAC technology.
Cell Rep, 2025, 44(6):115800
Cell Commun Signal, 2025, 23(1):364
Eur J Med Chem, 2024, 268:116202
S8975 Mezigdomide (CC-92480) Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
Nat Commun, 2024, 15(1):8885
Mol Cancer Ther, 2023, 22(5):659-666
Nature Communications, 15 October 2024, 8885

Signaling Pathway Map