MK2-IN-6 (Compound 11) is an effective and selective irreversible inhibitor of MK2 with an IC50 value of 2.3 nM. It suppresses the kinase activity of MK2, leading to sustained inhibition of MK2 signaling and reduction of pathological inflammatory factors in macrophages. MK2-IN-6 is capable of inhibiting the M2-like protein phenotype in macrophages both in vitro and in vivo, showing potential for use in colorectal cancer research.

p70S6Kb:>1000 nM, TTK:>1000 nM, MK3:>100 nM, FGFR4:>1000 nM, MK5:>100 nM, p38:>1000 nM

MK2-IN-6 显示了对 MK2 的高选择性和不可逆的抑制效果,其半抑制浓度为 2.3 nM,作用时间为 70 分钟,其抑制性能与 PF-3644022 相似.此外,MK2-IN-6 在浓度范围 1-10 μM,作用时间为 1.5 或 6 小时时,能有效抑制巨噬细胞中多种细胞因子的转录和生成,作用靶点为 MK2 的关键下游基因.

MK2-IN-6(10 mg/kg, 腹腔注射, 每日两次,连续12天)在MC38肿瘤模型小鼠中有效抑制了肿瘤的生长.