h929

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

PROTAC SMARCA2-degrader-36 (compound 38) is an SMARCA2 degrader that achieves a 99% degradation rate at 100 nM in H929 cells. It possesses antiproliferative activity and is used in cancer research.

PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

MGD-22 is a molecular glue and orally active degrader of IKZF1/2/3, with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. It exhibits strong anti-proliferative activity against various hematological cancer cells and induces cell apoptosis (apoptosis). MGD-22 demonstrates significant anti-tumor efficacy in mice with NCI-H929 or WSU-DLCL-2 xenografts. This compound is useful for researching blood cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).