| Bioactivity | CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research[1]. |
| Invitro | CLK1-IN-3 (compound 10ad) 由于对 Clk1 和 Clk2 具有双重抑制作用而显示出抗肿瘤潜力[1]。CLK1-IN-3 (1000 μM) 能有效结合Clk1蛋白并以剂量依赖的方式抑制其降解[1]。CLK1-IN-3 (0-10 μM, 24 h) 在 Hela、BNLCL.2 和 HCT 116 细胞中诱导自噬[1]。CLK1-IN-3 刺激 SQSTM1/p62（自溶酶体标志物）的降解[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | CLK1-IN-3 (compound 10ad) (0-40 mg/kg, 腹腔注射, 一次) 在acetaminophen (HY-66005, APAP) 诱导的 ALI 模型，可显著抑制急性肝损伤 (ALI)，且没有明显的肝细胞死亡[1].CLK1-IN-3 (10 mg/kg; 静脉注射, 口服, 腹腔注射, 一次) 表现出可接受的药代动力学特征，具有相对较长的 T1/2，为 5.29 小时，口服生物利用度为 19.5%[1]。 Animal Model: |
| Name | CLK1-IN-3 |
| Formula | C24H23FN6O |
| Molar Mass | 430.48 |
| 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]. Yang T, et al. Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI). Eur J Med Chem. 2023 Mar 15;250:115168. |