Bim Inhibitor

SHP2-D26 is a SHP2 PROTAC degrader with DC₅₀ values of 6.0 nM (KYSE520 cells) and 2.6 nM (MV4;11 cells), respectively. SHP2-D26 inhibits ERK phosphorylation, upregulates Bim levels, downregulates Mcl-1 levels, and induces cell cycle arrest and apoptosis. SHP2-D26 can be used in studies related to esophageal cancer, acute myeloid leukemia and non-small cell lung cancer.

Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.

BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a K_i of 2.4±0.2 μM in FP assay. BH3I-1 has a K_d of 5.3 μM against the p53/MDM2 pair.

ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.

Mcl-1-IN-23 is a Mcl-1 inhibitor with a K_i value of 0.024 μM. Mcl-1-IN-23 binds directly to Mcl-1 and displaces the pro-apoptotic proteins Bak and Bim from Mcl-1 complexes. Mcl-1-IN-23 induces cell apoptosis, activates caspase-3, promotes PARP cleavage, and exerts antiproliferative activity against cancer cells. Mcl-1-IN-23 can be used for the research of leukemia.