ikaros

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.

MGD-4 is an orally active, Cereblon (CRBN)-dependent degrader of IKAROS proteins that demonstrates dose-dependent degradation of IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM). The compound effectively inhibits the growth of multiple myeloma.

MS40 is a WDR5 PROTAC that selectively degrades WDR5 and serves as a novel degrader for immune-modulating compounds (IMiDs), including the new substrates CRBN and Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3. MS40 facilitates the degradation of WDR5, resulting in the dissociation of the MLL/KMT2A complex from chromatin, thereby reducing H3K4me2 levels. In vitro, MS40 inhibits the growth of primary leukemia patient cells, and in vivo, it suppresses the expansion of patient-derived xenografts.

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.

ALV1 is a molecular glue degrader that targets and degrades Ikaros (IKZF1) and Helios (IKZF2), with DC50 values of 2.5 nM and 10.3 nM, respectively. ALV1 binds to CRBN with an IC50 of 0.55 μM and induces the dimerization of CRBN and Helios. It can be used to investigate the properties and functions of regulatory T cells .

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.

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].

KTX-955, a potent IRAK4 degrader, exhibits DC50 values of 5 nM for IRAK4 and 130 nM for Ikaros. It is primarily utilized in anticancer research [1] [2].

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].