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E3 Ligase Inhibitors/Modulators

Other Ubiquitin Related Inhibitors

E1 Activating DUB E2 conjugating p97 SUMO

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.
Cell Rep Med, 2025, S2666-3791(25)00231-9
BMC Cancer, 2025, 25(1):1304
The Journal of Clinical Investigation, 2022-, -Volume 132, Issue 24
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.
Nature, 2025, 647(8091):952-961
Theranostics, 2025, 15(8):3439-3461
Cell Mol Biol Lett, 2025, 30(1):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.
bioRxiv, 2024, 10.1101/2024.01.28.577572
Cell Chem Biol, 2022, S2451-9456(22)00204-5
Leukemia, 2021, 35(5):1330-1343
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.
Nat Commun, 2023, 10.1038/s41467-023-42930-y
Leukemia, 2021, 10.1038/s41375-021-01121-8
J Exp Clin Cancer Res, 2021, 40(1):195
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
Int J Mol Sci, 2024, 25(16)8984
Molecules, 2024, 29(2)482
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
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.
J Immunother Cancer, 2024, 12(12)e009444
Cell Death Discov, 2023, 9(1):364
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

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