| 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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| E1184 |
CFT7455
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CFT7455 is an orally active zinc finger transcription factors (IKZF1) (Ikaros) and IKZF3 (Aiolos) degrader. It binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM). It is used in the treatment of multiple myeloma & non-Hodgkin’s lymphoma.
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| E1204 |
NVP-DKY709
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NVP-DKY709 is a potent IKZF2 inhibitor for the treatment of cancers.
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| S2881 |
Homo-PROTAC cereblon degrader 1
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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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Antimicrob Agents Chemother, 2025, 69(1):e0117224
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Eur J Immunol, 2021, 10.1002/eji.202149269
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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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| E1381 |
NX-2127
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NX-2127 is a unique, potent inhibitor of BTK that prevents its functions by catalyzing the ubiquitylation and proteasomal degradation of BTK rather than via direct binding. This compound stimulates T cell activation and increases IL-2 production in primary human T Cells.
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| E4669New |
KT-413
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KT-413 (IRAK degrader-1, zomiradomide) is a dual-function PROTAC molecule and a potent degrader of interleukin-1 receptor associated kinase 4 (IRAK4) and the transcription factors Ikaros and Aiolos by acting as both a heterobifunctional degrader and a molecular glue. It can be used in research for developing therapies targeting the activated B-cell (ABC) subtype of diffuse large B-cell lymphoma (DLBCL).
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| E6029 |
Lenalidomide hemihydrate
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Lenalidomide hemihydrate (CC-5013 hemihydrate) is a potent inhibitor of TNF-alpha with a IC50 of 13 nM. It induces tyrosine phosphorylation of CD28 on T cells, which subsequently activates NF-κB. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), leading to the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex.
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| E4724New |
MGD-28
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MGD-28 is a potent and orally active degrader of Cereblon (CRBN)-dependent IKAROS proteins. It effectively degrades IKZF1 (DC50 = 3.8 nM), IKZF2 (DC50 = 56.3 nM), and IKZF3 (DC50 = 7.1 nM). It demonstrates significant antiproliferative potency across various hematologic cancer cell lines.
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