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 是一种 PD-1/PD-L1 免疫检查点抑制剂，对 PD-L1/PD-1 复合物的 IC50 为 18–200 nM，同时对改造的 Jurkat T 细胞表现出非特异性细胞毒性（EC50 为 3–6 μM）。BMS-37 广泛用于研究 PD-L1 诱导的 T 细胞耗竭机制，或作为 PD-L1 配体骨架用于免疫肿瘤学中 PROTAC 分子的理性设计与合成。