E3 Ligase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
Eur J Immunol, 2021, 10.1002/eji.202149269
S8300 CC-885

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

Sci Rep, 2025, 15(1):2384
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.
E1427 MRT-2359 MRT-2359 is a potent degrader of GSPT1. It exhibits anti-tumour activity in non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells.
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.
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 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.
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.
E5839New 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.
E5877New 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 leukaemia 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.
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)
S1172 Serdemetan (JNJ-26854165) Serdemetan (JNJ-26854165) acts as an HDM2 ubiquitin E3 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)
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.
Cell Death Discov, 2024, 10(1):381
J Cancer, 2023, 14(2):200-218
Theranostics, 2022, 12(9):4110-4126
Verified customer review of RITA
S2225 TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
Dev Cell, 2023, 58(3):192-210.e11
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.
PLoS One, 2024, 19(1):e0295629
Front Oncol, 2021, 11:582511
Genes Dev, 2020, 34(7-8):526-543
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).