celmod

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue. Mezigdomide has anti-myeloma activity. [1]

BMS-986449 is an IKZF2 (Helios)/IKZF4 (Eos) degrader and CELMoD molecular glue. It redirects the interaction between the E3 ubiquitin ligase Cereblon and Helios/Eos in primary Treg cells, inducing their degradation, and may be utilised for anti-tumour immunotherapy.

BMS-986470 is a CRBN E3 ubiquitin ligase modulator (CELMoD) that activates fetal hemoglobin (HbF). It is an orally available molecular glue degradator targeting ZBTB7A and WIZ protein degradation, thereby inducing gamma globin synthesis and activating HbF. It is applicable for studying sickle cell disease (SCD).

BMS-986463 is a WEE1 kinase molecule gel degrader and a CRBN E3 ligase regulator (CELMoD). BMS-986463 significantly inhibits tumor regression and reduces the level of phosphorylated CDK2. BMS-986463 is utilized in oncology research involving cell-cycle checkpoint regulation, protein degradation pathways, and malignant solid tumor models including non-small cell lung cancer (NSCLC).

BMS-986482 is a novel Cereblon (CRBN) E3 ubiquitin ligase modulator (CELMoD) and targeted proteolytic agent that also exerts antitumor activity by degrading proteins of the IKZF family of transcription factors (IKZF1–4) as a “Molecular Glue” degrader. In preclinical mouse models, it inhibits tumor growth as a single agent. BMS-986482 exhibits antiproliferative and immunomodulatory activity in hematologic malignancies and solid tumor models and is currently in Phase I/II clinical trials for advanced solid tumors.

(R)-BMS-986470 is the enantiomer of BMS-986470. BMS-986470 functions as a CRBN E3 ligase modulator (CELMoD) that activates HbF. It is an orally active, dual molecular glue degrader targeting ZBTB7A and WIZ.