E3 Ligase Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S8449 | VH298 | VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilises 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 polarisation assay. It can be used in PROTAC technology. |
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| 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. |
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| 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. |
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| 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 stabilising HIF-α, it activates the hypoxic response and serves as a tool for developing therapies targeting hypoxia signalling. | ||
| 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-tumour 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 tumour 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 potentially 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. |
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| 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. |
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| 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. |
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| S2225 | TAME | Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor. |
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| 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). |
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