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E3 Ligase

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E3 Ligase Signaling Pathway Map

Isoform-selective Inhibitors

CRBN Selective

E3 Ligase Products

All (30)
E3 Ligase Inhibitors (17)
E3 Ligase Activators (2)
E3 Ligase Antagonists (2)
E3 Ligase Modulators (2)
New E3 Ligase Products

Catalog No.	Product Name	Information	Product Use Citations
E0351^New	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.
E1087^New	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.	Genes Dev, 2020, 34(7-8):526-543 Oncotarget, 2020, 11(46):4224-4242 Sci Rep, 2019, 9(1):1897
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 CRL4^CRBN.	Leukemia, 2021, 35(5):1330-1343 Mol Ther Oncolytics, 2020, 18:215-225 Blood Adv, 2019, 3(14):2105-2117
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^New	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.
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.	Cancer Cell, 2020, S1535-6108(20)30605-X Cancers (Basel), 2020, 12(9)E2668 Cancer Discov, 2020, CD-20-0160
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 K_i 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^New	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.
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.	Nat Commun, 2022, 13(1):1009 Theranostics, 2022, 12(4):1715-1729 Cell Death Dis, 2022, 13(3):197
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 an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
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 Mol Cancer Ther, 2022, molcanther.0835.2021 Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.	Pharmaceuticals (Basel), 2022, 15(2)241 Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831 Hemasphere, 2021, 5(7):e602
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.
E0351^New	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.
E1087^New	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.	Genes Dev, 2020, 34(7-8):526-543 Oncotarget, 2020, 11(46):4224-4242 Sci Rep, 2019, 9(1):1897
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 CRL4^CRBN.	Leukemia, 2021, 35(5):1330-1343 Mol Ther Oncolytics, 2020, 18:215-225 Blood Adv, 2019, 3(14):2105-2117
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^New	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.
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.	Cancer Cell, 2020, S1535-6108(20)30605-X Cancers (Basel), 2020, 12(9)E2668 Cancer Discov, 2020, CD-20-0160
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 K_i 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^New	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.
E0351^New	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.
E1087^New	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.
S9832^New	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.
S8300^New	CC-885	CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation.

Tags: Ubiquitin ligase inhibitor | E3 ligase inhibitor