mm1.s

Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis.

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

Biotinylated-JQ1 (Biotin-JQ1), a biotinylated derivative of JQ1, selectively binds to the BRD4 bromodomain with high affinity. It effectively inhibits the proliferation of MM1.S multiple myeloma cells, demonstrating an EC50 of 0.4 μM [1].

ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].