aiolos

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

MGD-28 is a potent, orally active Cullin-CRBN-dependent IKZF family protein degrader that dose-dependently degrades IKZF1 (Ikaros), IKZF2 (Helios), and IKZF3 (Aiolos) at nanomolar strengths.MGD-28 also degrades CK1α, and has shown antiproliferative activity against a variety of hematologic cancer cell lines showing antiproliferative activity in vitro and antitumor effects in in vivo assays, and is commonly used in multiple myeloma (MM) and hematological disorders.

BMS-986458 is an oral heterobifunctional degrader that targets the Cereblon (CRBN) E3 ubiquitin ligase. By binding to the BTB domain of BCL6, it induces the formation of a ternary complex between BCL6 and CRBN, thereby promoting the ubiquitination and proteasomal degradation of BCL6. BMS-986458 exhibits high selectivity for BCL6 degradation while showing weak degradation activity toward known new CRBN substrates (such as Ikaros, Aiolos, SALL4, and GSPT1), making it a valuable tool for studying BCL6-related tumor signaling pathways and antitumor mechanisms.

Avadomide is an orally available pleiotropic pathway modulator with potential antineoplastic activity. CC-122 mimics an interferon response and has antitumor activity in DLBCL CC-122 binds Cereblon (CRBN) and promotes degradation of Ikaros and Aiolos in d

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).

(Rac)-CFT7455 is an Ikaros/Aiolos degradation agent that acts via the ubiquitin proteasome pathway and is able to act on NCIH929.1 cells (GI50: 0.05 nM). (Rac)-CFT7455 is a racemic isomer of CFT7455 and has anticancer activity.

NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative activity and inhibits the proliferation of BTKC481S mutant TMD8 cells.NX-2127 potently catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) at 25 nM and 54 nM, respectively. NX-2127 is associated with the immune system, stimulating T cell activation and increasing IL-2 production in primary human T cells.

Zomiradomide is a PROTAC degradation agent targeting IRAK4, with oral bioavailability, and can also degrade Ikaros (IKZF1) and Aiolos (IKZF3), thereby inhibiting the NF-κB signalling pathway and activating the type I interferon signalling pathway, exhibiting anticancer activity against B-cell lymphoma.

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].