ly-3325656

LY3325656 is a GPR142 agonist suitable for clinical testing in human. LY3325656 demonstrated anti-diabetic benefits in pre-clinical studies and ADME PK properties suitable for human dosing. LY3325656 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.

APS-2-79 是一种 KSR 依赖性的MEK 拮抗剂。APS-2-79 与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的KSR2，IC50为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态，使其无法再结合RAF 和激活MEK，从而阻断了 Ras-MAPK 信号通路。