UK-5099 (PF-1005023) is an inhibitor of the mitochondrial pyruvate transporter protein MPC. UK-5099 inhibits MPC by covalently and reversibly binding to the C54 of MPC2, which facilitates the transport of pyruvate across the inner mitochondrial membrane. UK-5099 has antitumor activity.

MPC:50 nM

方法：大鼠胰岛素瘤细胞 832/13 用 glucose (2-8 mM) 和 UK-5099 (10-150 µM) 处理 2 h，使用 Coat-A-Count radioimmunoassay kit 检测细胞胰岛素分泌。
结果：UK-5099 对基础胰岛素分泌没有显著影响。在使用 UK-5099 的 832/13 细胞中，在 6 和 8 mM glucose 下对胰岛素分泌显示出更一致的抑制作用。[1]
方法：人前列腺癌细胞 LnCap 用 UK-5099 (10 µM) 处理 1-5 天，使用 trypan blue dye 检测细胞数目。
结果：UK-5099 抑制了 LnCap 细胞的细胞增殖。[2]

方法：为研究在体内葡萄糖耐量中发挥的作用，将 UK-5099 (32 µmol/kg) 单次腹腔注射给进行葡萄糖耐量试验的 C57BLK 小鼠。
结果：UK-5099 在 30、60 和 120 min 时引起显著更大的葡萄糖漂移。UK-5099 也显著增加了曲线下面积。这些研究表明 MPC 在体内调节葡萄糖耐量方面发挥着重要作用。[1]

The 832/13 cell line derived from INS-1 rat insulinoma cells is used for experiments. Cell viability is measured using CellTiter Blue. The assay is based on the cellular reduction of resazurin to resorufin. The appearance of resorufin is monitored by fluorescence emission at 585 nm using a Spectramax M5 microplate reader with excitation at 555 nm. For UK5099-treated cells, cells are allowed to recover for 1 h before measuring cell viability. Data are expressed as -fold relative to no treatment or siCtrl[4].

C57BLK mice are fasted for 16 h prior to glucose challenge. UK5099 (32 μmol/kg of body weight) or DMSO in PBS is injected into the intraperitoneal cavity 30 min before injecting glucose (1.5 mg of glucose/g of body weight). Blood glucose levels are measured at 0, 10, 20, 30, 60, and 120 min after glucose injection[4].