| 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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| 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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| 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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