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E3 Ligase
Isoform-selective Products
Signaling Pathway
E3 Ligase Products
- All (40)
- E3 Ligase Inhibitors (28)
- E3 Ligase Activator (1)
- E3 Ligase Antagonists (2)
- E3 Ligase Modulators (3)
- New E3 Ligase Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S1029 | Lenalidomide | Lenalidomide 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. |
|
|
| S1567 | Pomalidomide | Pomalidomide 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S1193 | Thalidomide | Thalidomide 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. |
|
|
| 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. |
|
|
| S2225 | TAME | Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor. |
|
|
| S2781 | RITA | RITA 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S8975 | Mezigdomide (CC-92480) | Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity. | ||
| 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. | ||
| S4925New | 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. | ||
| E1427 | MRT-2359 | MRT-2359 is a potent degrader of GSPT1. It exhibits anti-tumor activity in non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells. | ||
| E1957New | NX-1607 | 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. | ||
| S8300 | CC-885 | CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation. |
||
| 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. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6. | ||
| 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. | ||
| E1847New | GBD-9 | GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1.It exhibits anti-proliferative effects, inhibiting cancer cell survival. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E1300 | SJ6986 | SJ6986 is a CRBN modulator and specifically degrades GSPT1/2, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1. | ||
| 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. | ||
| E1937New | PT-179 | PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 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. | ||
| 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. | ||
| 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). | ||
| 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. NSC232003 modulates DNA methylation in a cellular context. | ||
| E1678New | 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. | ||
| 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). | ||
| 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. |
||
| S1029 | Lenalidomide | Lenalidomide 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. |
|
|
| S1567 | Pomalidomide | Pomalidomide 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. |
|
|
| 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. |
|
|
| S1193 | Thalidomide | Thalidomide 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. |
|
|
| S2225 | TAME | Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor. |
|
|
| S2781 | RITA | RITA 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S4925New | 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. | ||
| E1957New | NX-1607 | 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. | ||
| 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. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E1937New | PT-179 | PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 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. | ||
| 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). | ||
| 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. NSC232003 modulates DNA methylation in a cellular context. | ||
| E1678New | 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. |
||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S8975 | Mezigdomide (CC-92480) | Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity. | ||
| S8300 | CC-885 | CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation. |
||
| E1300 | SJ6986 | SJ6986 is a CRBN modulator and specifically degrades GSPT1/2, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1. | ||
| S4925New | 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. | ||
| E1957New | NX-1607 | 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. | ||
| E1847New | GBD-9 | GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1.It exhibits anti-proliferative effects, inhibiting cancer cell survival. | ||
| E1937New | PT-179 | PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 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. | ||
| E1678New | 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. |
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Tags: Ubiquitin ligase inhibitor | E3 ligase inhibitor
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