ikaros

E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.

CFT7455 (Cemsidomide) is an anti-cancer agent showing high affinity to the cereblon E3 ligase with a Kd of 0.9 nM. CFT7455 is an orally active degrader of zinc finger transcription factors Ikaros (IKZF1), and Aiolos (IKZF3).

ALV1 is a potent degradation agent of Ikaros and Helios, with similar degradation activity against IKZF1 2 3. ALV1 significantly reduced the protein abundance of IKZF1-4, CK1α (casein kinase 1α, CSNK1A1) and ribosomal protein RPL4, and induced Helios CRBN dimerization, which promoted IL-2 secretion.

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

E3 Ligase Ligand 21 (compound 2), a cereblon binder, facilitates the degradation of Ikaros or Aiolos via the ubiquitin proteasome pathway [1].

E3 Ligase Ligand 22 (compound 139) serves as a cereblon binder, facilitating the degradation of Ikaros or Aiolos via the ubiquitin proteasome pathway [1].