bms-186511.

BMS-186511 is a Farnesyltransferase (FT) inhibitor with potential anticancer activity. BMS-186511 is a bisubstrate analogue inhibitor of FT, would inhibit the malignant growth properties of a cell line established from malignant schwannoma of an NF1 patient. Following treatment with BMS-186511 , ST88-14 cells became flat, nonrefractile, were contact-inhibited, and lost their ability to grow in soft agar. BMS-186511 was found to specifically inhibit FT, but not geranylgeranyltransferase I, a closely related enzyme. Thus, it is conceivable that FT inhibitors may ultimately become the first generation of drugs against the malignant phenotype in NF1 based on rational insights into the mechanism of action of neurofibromin.

BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor exhibiting IC50 values ranging from 18 to 200 nM against the PD-L1/PD-1 complex, while displaying nonspecific cytotoxicity toward modified Jurkat T cells with EC50 values between 3 and 6 μM, and it is widely used to investigate PD-L1–induced T-cell exhaustion mechanisms or as a PD-L1 ligand scaffold for the rational design and synthesis of PROTAC molecules in immuno-oncology research.