| Bioactivity | MK2-IN-6 (Compound 11) is a potent and selective irreversible MK2 inhibitor with an IC50 value of 2.3 nM. MK2-IN-6 inhibits MK2 kinase activity, achieving prolonged MK2 signaling suppression and reducing pathological inflammatory cytokines in macrophages. MK2-IN-6 inhibits the M2-like protumor phenotype of macrophages both in vitro and in vivo, which is proming for research of colorectal cancer[1]. |
| Invitro | MK2-IN-6 (2.3 nM, 70 分钟) 对 MK2 具有高选择性和不可逆的抑制作用，类似 PF-3644022 (HY-107427)[1]。MK2-IN-6 (1-10 μM, 1.5 或 6 小时) 可深度抑制巨噬细胞中细胞因子的转录和产生，靶向 MK2 的经典下游基因[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> MK2-IN-6 相关抗体: Real Time qPCR[1] Cell Line: |
| In Vivo | MK2-IN-6 (10 mg/kg, 腹腔注射, 每天两次，持续 12 天) 显著抑制 MC38 肿瘤模型小鼠的肿瘤生长[1]。MK2-IN-6 在小鼠体内的药动学参数[1]药代动力学分析[1]ip. (10 mg/kg) |
| Formula | C22H17F3N4O3 |
| Molar Mass | 442.39 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang D, et al. Remodeling tumor-associated macrophage for anti-cancer effects by rational design of irreversible inhibition of mitogen-activated protein kinase-activated protein kinase 2[J]. MedComm (2020). 2024 Jul 10;5(7):e634. |