SHP2-IN-42 is an inhibitor of the phosphatase containing the Src homology 2 domain (SHP2), with an IC50 of 15 nM. It inhibits cell proliferation, induces apoptosis, and causes G1 phase cell cycle arrest. SHP2-IN-42 is applicable in cancer research, including studies on acute myeloid leukemia (AML).

SHP2:15 nM

SHP2-IN-42 (Compound B8) inhibits cell proliferation with an IC50 of 4.96 μM in MV4-11 cells and 4.25 μM in MOLM-13 cells. It induces apoptosis in MOLM-13 cells at concentrations of 2.5-10 μM over 48 hours. At the same concentration range, it causes G1 phase cell cycle arrest in MOLM-13 cells within 24 hours and reduces ERK phosphorylation levels after 3 hours. Additionally, when used in combination with MCL-1 inhibitor VU661013 at 3-6 μM over 24 hours, it induces mitochondrial membrane potential disruption and activates apoptosis in MOLM-13 cells.