E3 Ligase

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E3 Ligase Signaling Pathway Map

E3 Ligase  Signaling Pathways
Isoform-selective Inhibitors

E3 Ligase Products

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  • E3 Ligase Inhibitors (19)
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  • E3 Ligase Antagonists (2)
  • E3 Ligase Modulators (2)
  • New E3 Ligase Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0071New 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.
E0351New NSC232003 NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor that binds to the 5mC binding pocket of the SRA domain of UHRF1. NSC232003 modulates DNA methylation in a cellular context.
E1087New 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.

S0095 VL285 VL285 is a potent VHL ligand that degrades HaloTag7 fusion proteins. Cotreatment with excess VL285, the core VHL ligand from which HaloPROTAC3 is derived, is able to significantly reduce HaloPROTAC3 mediated activity to 50% 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.
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. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6.
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.
S2225 TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep, 2021, 34(10):108814
Hum Cell, 2021, 34(6):1911-1918
S2678 NSC 207895 NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
Front Oncol, 2021, 11:582511
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
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.
Eur J Immunol, 2021, 10.1002/eji.202149269
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.
Leukemia, 2021, 10.1038/s41375-021-01121-8
J Exp Clin Cancer Res, 2021, 40(1):195
Leukemia, 2021, 10.1038/s41375-021-01121-8
S7892 Avadomide (CC-122) Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is 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.
Cell Chem Biol, 2022, S2451-9456(22)00204-5
Leukemia, 2021, 35(5):1330-1343
Mol Ther Oncolytics, 2020, 18:215-225
S8449 VH298 VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 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. VH-298 can be used in PROTAC technology.
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.
Pharmaceuticals (Basel), 2022, 15(2)241
Cancer Discov, 2021, candisc.0209.2021
Eur Rev Med Pharmacol Sci, 2020, 24(6):2802-2810
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 a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
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.
Prostate, 2021, 10.1002/pros.24257
Breast Cancer, 2021, 10.1007/s12282-021-01242-z
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. SZL P1-41 causes higher apoptosis rates in cancer cells.
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.
S9889New 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.
A5316 PIAS1/PIAS2/PIAS3 Rabbit Recombinant mAb PIAS1/PIAS2/PIAS3 Rabbit Recombinant mAb detects endogenous level of total PIAS1/PIAS2/PIAS3.
S1172 Serdemetan (JNJ-26854165) Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.
Signal Transduct Target Ther, 2022, 7(1):97
iScience, 2021, 24(9):103080
Cancer Res, 2020, canres.3499.2019
S2781 RITA (NSC 652287) RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.
Theranostics, 2022, 12(9):4110-4126
Cancer Cell, 2020, S1535-6108(20)30605-X
Cancers (Basel), 2020, 12(9)E2668
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.
Nat Biotechnol, 2022, 10.1038/s41587-021-01172-3
Cell Death Differ, 2022, 10.1038/s41418-022-00992-3
J Exp Clin Cancer Res, 2022, 41(1):79
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.
Theranostics, 2021, 11(18):9009-9021
Cancers (Basel), 2021, 13(14)3585
Neoplasia, 2021, 23(5):539-550
S8300 CC-885

CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation.

S8975 Mezigdomide (CC-92480) Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
S1015 Thalidomide-OH Thalidomide-OH (Cereblon ligand 2, E3 ligase Ligand 2) is a presumed hydroxylated thalidomide metabolite, with weak antiangiogenic activity (the average inhibition rate of vessel density was 14% in 100 μg), also can be applicable to the recruitment of CRBN protein.
S1029 Lenalidomide (CC-5013) Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Cancer Cell, 2022, S1535-6108(22)00312-9
Nat Commun, 2022, 13(1):1009
Theranostics, 2022, 12(4):1715-1729
S1193 Thalidomide (K17) Thalidomide (K17) was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.
Cell Chem Biol, 2022, S2451-9456(22)00204-5
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1567 Pomalidomide (CC-4047) Pomalidomide (CC-4047) inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
Nat Commun, 2022, 13(1):1009
Cell Chem Biol, 2022, S2451-9456(22)00204-5
Mol Cancer Ther, 2022, molcanther.0835.2021
S3502 (S,R,S)-AHPC-PEG4-NH2 hydrochloride (S,R,S)-AHPC-PEG4-NH2 hydrochloride (VH032-PEG4-NH2 hydrochloride, VHL Ligand-Linker Conjugates 4 hydrochloride, E3 ligase Ligand-Linker Conjugates 7) is a PROTAC E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker.
S6794 Thalidomide-O-COOH (Cereblon ligand 3) Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase Ligand 3), a Thalidomide-based Cereblon (CRBN) ligand, is used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera).
S8760 Iberdomide (CC220) 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 Chem Biol, 2022, S2451-9456(22)00204-5
Pharmaceuticals (Basel), 2022, 15(2)241
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831
S8888 GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
E0071New 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.
E0351New NSC232003 NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor that binds to the 5mC binding pocket of the SRA domain of UHRF1. NSC232003 modulates DNA methylation in a cellular context.
E1087New 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.

S0095 VL285 VL285 is a potent VHL ligand that degrades HaloTag7 fusion proteins. Cotreatment with excess VL285, the core VHL ligand from which HaloPROTAC3 is derived, is able to significantly reduce HaloPROTAC3 mediated activity to 50% 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.
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. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6.
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.
S2225 TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep, 2021, 34(10):108814
Hum Cell, 2021, 34(6):1911-1918
S2678 NSC 207895 NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
Front Oncol, 2021, 11:582511
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
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.
Eur J Immunol, 2021, 10.1002/eji.202149269
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.
Leukemia, 2021, 10.1038/s41375-021-01121-8
J Exp Clin Cancer Res, 2021, 40(1):195
Leukemia, 2021, 10.1038/s41375-021-01121-8
S7892 Avadomide (CC-122) Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is 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.
Cell Chem Biol, 2022, S2451-9456(22)00204-5
Leukemia, 2021, 35(5):1330-1343
Mol Ther Oncolytics, 2020, 18:215-225
S8449 VH298 VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 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. VH-298 can be used in PROTAC technology.
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.
Pharmaceuticals (Basel), 2022, 15(2)241
Cancer Discov, 2021, candisc.0209.2021
Eur Rev Med Pharmacol Sci, 2020, 24(6):2802-2810
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 a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
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.
Prostate, 2021, 10.1002/pros.24257
Breast Cancer, 2021, 10.1007/s12282-021-01242-z
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. SZL P1-41 causes higher apoptosis rates in cancer cells.
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.
S9889New 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.
A5316 PIAS1/PIAS2/PIAS3 Rabbit Recombinant mAb PIAS1/PIAS2/PIAS3 Rabbit Recombinant mAb detects endogenous level of total PIAS1/PIAS2/PIAS3.
S1172 Serdemetan (JNJ-26854165) Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.
Signal Transduct Target Ther, 2022, 7(1):97
iScience, 2021, 24(9):103080
Cancer Res, 2020, canres.3499.2019
S2781 RITA (NSC 652287) RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.
Theranostics, 2022, 12(9):4110-4126
Cancer Cell, 2020, S1535-6108(20)30605-X
Cancers (Basel), 2020, 12(9)E2668
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.
Nat Biotechnol, 2022, 10.1038/s41587-021-01172-3
Cell Death Differ, 2022, 10.1038/s41418-022-00992-3
J Exp Clin Cancer Res, 2022, 41(1):79
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.
Theranostics, 2021, 11(18):9009-9021
Cancers (Basel), 2021, 13(14)3585
Neoplasia, 2021, 23(5):539-550
S8300 CC-885

CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation.

S8975 Mezigdomide (CC-92480) Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
E0071New 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.
E0351New NSC232003 NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor that binds to the 5mC binding pocket of the SRA domain of UHRF1. NSC232003 modulates DNA methylation in a cellular context.
E1087New 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.

S9889New 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.
Tags: Ubiquitin ligase inhibitor | E3 ligase inhibitor