| S1029 |
CC-5013 (Lenalidomide)
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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.
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Signal Transduct Target Ther, 2025, 10(1):29
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Nat Commun, 2025, 16(1):3800
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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| S1567 |
Pomalidomide (CC-4047)
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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.
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Nat Commun, 2025, 16(1):6631
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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J Med Virol, 2025, 97(8):e70537
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| S8760 |
Iberdomide (CC-220)
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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.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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J Med Virol, 2025, 97(8):e70537
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Cancer Res, 2025, 10.1158/0008-5472.CAN-24-1136
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| E5871New |
VAV1 degrader-3
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VAV1 degrader-3 (MRT-6160) is an orally active molecular glue degrader of VAV1 with a DC50 of 7 nM. It suppresses immune activation, proliferation, and cytokine production, inhibiting disease progression in inflammatory and autoimmune models like encephalomyelitis (EAE) and Collagen-induced arthritis (CIA).
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| E5854New |
XYD049
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XYD049 (compound 7d) is a CRBN-based molecular glue targeting GSPT1 (DC50=19 nM), applicable for studying MYC-driven castration-resistant prostate cancer (CRPC). It demonstrates potent growth inhibition of 22Rv1 cells (IC50=7 nM) and exhibits in vivo antitumor activity. This compound downregulates CRPC-associated oncogenes (AR, AR-v7, PSA, c-Myc) in 22Rv1 cells. Structurally, it consists of: 1) a molecular glue linker (NH2-C5-NH-Boc), 2) a CRBN-recruiting E3 ligase ligand (Thalidomide 4-fluoride), and 3) a GSPT1-targeting moiety (GSPT1 ligand-1). The E3 ligase ligand-linker combination forms conjugate 158.
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| E1810 |
dCeMM1
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dCeMM1 is a degrader of RBM39. This compound functions by altering the activity of the CRL4DCAF15 ligase, and also decreases RBM39 expression levels in wild-type KBM7 cells.
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| S1193 |
Thalidomide
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Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. This compound inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.
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Nat Genet, 2025, 57(10):2468-2481
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Biomed Pharmacother, 2025, 184:117878
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Nat Commun, 2024, 15(1):9195
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| S8975 |
Mezigdomide (CC-92480)
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Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.
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Nat Commun, 2024, 15(1):8885
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Mol Cancer Ther, 2023, 22(5):659-666
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Mol Cancer Ther, 2023, 22(5):659-666
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| E1427 |
MRT-2359
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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.
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| E1413 |
DEG-77
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DEG-77 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.
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