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E3 Ligase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
S2881 Homo-PROTAC cereblon degrader 1 Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
Antimicrob Agents Chemother, 2025, 69(1):e0117224
Eur J Immunol, 2021, 10.1002/eji.202149269
S4925 SMER3 SMER3, the small-molecule enhancer of rapamycin (SMER), is an inhibitor of the Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase with IC50 of 51 nM.
E7042 SMIP004 SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
E7619 VH032 VH032 is a potent and selective VHL ligand used in PROTACs that binds to the VHL E3 ligase with a Kd of 185 nM and disrupts the VHL:HIF-α interaction. By stabilizing HIF-α, it activates the hypoxic response and serves as a tool for developing therapies targeting hypoxia signaling.
E1957 NX-1607 (Cbl-b-IN-3) NX-1607 (Cbl-b-IN-3) is an oral inhibitor of Casitas B-lineage lymphoma proto-oncogene B (CBL-B), which is an E3 ubiquitin ligase and a key regulator of T, NK, and dendritic cell activation and suppresses their anti-tumor functions. NX-1607 enhances antigen recall, reduces T cell exhaustion, and increases cytokine production in response to T cell receptor stimulation, thereby counteracting suppressive signals from the tumor microenvironment.
E1216 Heclin Heclin is an inhibitor of HECT-type E3 ubiquitin ligase with an IC50 of 6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT domains, respectively.
S9889 dCBP-1 dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.
S0322 BC-1215 BC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. This compound inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6.
E5844New NSC2805 NSC2805 is a potent inhibitor of WWP2 ubiquitin ligase with an IC50 of 0.38 μM. It is used in cancer research for studying WWP2-associated pathways.
S9832 CC-90009 CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation.
S0097 (S,R,S)-AHPC (MDK7526) (S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.
S0345 Smurf1-IN-A01 Smurf1-IN-A01 can inhibit Smurf1-mediated Smad1/5 degradation and accelerate BMP-2 signal responsiveness with a Kd of 3.664 nM.
E0071 MuRF1-IN-1 MuRF1-IN-1 is a muscle ring finger protein-1 (MuRF1) inhibitor that attenuates skeletal muscle atrophy and dysfunction in cardiac cachexia.
E1937 PT-179 PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. This compound specifically binds CRBN, forms a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediates the degradation of the tagged protein.
E0351 NSC232003 NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor that binds to the 5mC binding pocket of the SRA domain of UHRF1. This compound modulates DNA methylation in a cellular context.
E1678 SPOP-i-6lc SPOP-i-6lc is a selective speckle-type POZ protein (SPOP) E3 ubiquitin ligase inhibitor with IC50 of 2.1 μM and 3.5 μM, in A498 and OS-RC-2 cell lines, respectively. In vitro, It suppresses viability and proliferation of A498 and OS-RC-2 kidney cancer cell lines.
E1087 5-amino-2,4-dimethylpyridine (5A-DMP)

5-amino-2,4-dimethylpyridine (5A-DMP) is a novel tandem Tudor domain (TTD)-binding compound that inhibits the full-length UHRF1:LIG1 interaction in Xenopus egg extracts.
S2754 Xevinapant (AT406) Xevinapant (AT406, ARRY-334543, Debio1143, SM-406) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.
Nat Commun, 2025, 16(1):2572
Cell Death Dis, 2025, 16(1):476
bioRxiv, 2025, 2025.09.22.677496
Verified customer review of Xevinapant (AT406)
S2781 RITA RITA induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and this compound also inhibits MDM2-p53 interaction by targeting p53.
Cell Death Discov, 2024, 10(1):381
J Cancer, 2023, 14(2):200-218
Theranostics, 2022, 12(9):4110-4126
Verified customer review of RITA
S2225 TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
Dev Cell, 2023, 58(3):192-210.e11
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Verified customer review of TAME
S8979 THAL-SNS-032 THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to that binds the E3 ubiquitin ligase Cereblon (CRBN).
Gastroenterology, 2024, S0016-5085(24)00062-3