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E3 Ligase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S8975 Mezigdomide (CC-92480) Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
Nat Commun, 2024, 15(1):8885
Mol Cancer Ther, 2023, 22(5):659-666
Nature Communications, 15 October 2024, 8885
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
Scientific Reports, 2025, 2384
European Journal of Immunology, 2021, 2607-2617
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.
Nature Communications, 2018, 1655
Frontiers in Immunology, 2018, 279
S8300 CC-885

CC-885 is a novel cereblon (CRBN) modulator. This compound selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation.
ACS Chemical Biology, November 3, 2022, 3229-3237
Sci Rep, 2025, 15(1):2384
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.
Neoplasia, 2022, 100784
E6808New PRLX-93936 hydrochloride PRLX-93936 hydrochloride is a potent molecular glue degrader that selectively binds to E3 ubiquitin ligase TRIM21 and forms a functional ternary complex between TRIM21 and NUP98 (Nucleoporin 98). This complex formation drives the subsequent polyubiquitination and proteasomal degradation of NUP98 alongside other essential components of the nuclear pore complex (NPC).
E6809New JWZ-8-103 JWZ-8-103 is an orally bioavailable selective degrader of the nuclear pore complex that acts as a TRIM21-targeting molecular glue. It induces a robust TRIM21 PRYSPRY–NUP98 APD interaction with an apparent EC50 ≈ 20 µM and increases TRIM21 thermal stability. It also exhibits potent antitumor efficacy in pancreatic cancer xenografts and patient-derived organoids.
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.
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.
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.
E5844 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.
E1847 GBD-9 GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). This compound 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.
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.
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.
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.
E6651New HGC652 HGC652 is a TRIM21-dependent molecular glue degrader that binds the E3 ubiquitin ligase TRIM21 (Kd ≈ 0.06 µM) to induce a TRIM21–NUP98 ternary complex, driving the ubiquitination and selective degradation of nuclear pore complex proteins like NUP155, leading to nuclear pore collapse and cancer cell death.
E5839 OICR-8268 OICR-8268 is a potent, reversible and in-cell active DCAF1 ligand. It significantly binds to DCAF1 WDR domain with an Kd value of 38 nM. It serves as a promising starting point for developing chemical handles for DCAF1-based PROTACs targeting selective protein degradation as well as cancer therapeutics.
E5877 LYG-409 LYG-409 is a potent, selective, and orally bioavailable degrader of GSPT1, with a DC50 of 7.87 nM. It exhibits strong antiproliferative activity in KG-1 cells with an IC50 of 9.50 nM and demonstrates significant antitumor efficacy in vivo in models of acute myeloid leukemia and prostate cancer.
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.
E6741New SB-405483 SB‑405483 is an allosteric cereblon (CRBN) ligand that cooperatively enhances the binding of orthosteric CRBN ligands (IMiDs) and potentiates degradation of CRBN neosubstrates, including CK1α, Wee1, and IKZF1/3. SB‑405483 stabilizes CRBN and reduces its autoubiquitination.
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.
PLOS ONE, 2026, e0343551
PLoS One, 2026, 21(2):e0343551
Cell Death Discov, 2024, 10(1):381
Verified customer review of RITA
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.
Elife, 2025, 14e75393
J Physiol, 2025, 603(19):5477-5508
Signal Transduct Target Ther, 2022, 7(1):97
Verified customer review of Serdemetan (JNJ-26854165)
S2225 TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
Oncotarget, May 3, 2016, 25478-25492
Dev Cell, 2023, 58(3):192-210.e11
J Pers Med, 2022, 12(2)258
Verified customer review of TAME
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.
Oncotarget, November 17, 2020, 4224-4242
PLoS One, January 26, 2024, e0295629
PLoS One, 2024, e0295629
Verified customer review of NSC 207895
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
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.
S6794 Thalidomide-O-COOH (Cereblon ligand 3) Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase Ligand 3), a Thalidomide-based Cereblon (CRBN) ligand used in the recruitment of CRBN protein, can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera).