G007-LK effectively inhibits TNKS1 and TNKS2, with IC50 values of 46 nM and 25 nM, respectively, and demonstrates a cellular IC50 of 50 nM. It does not inhibit PARP1 at concentrations up to 20 μM and possesses a high IC50 value for CYP3A4 inhibition (>25 μM)[1]. G007-LK (0-20 μM) inhibits the growth of hepatocellular carcinoma (HCC) cells in a dose-dependent manner. It reduces YAP levels by increasing AMOTL1 and AMOTL2 in HCC cell lines. Moreover, G007-LK (0-20 μM) works in synergy with MEK and AKT inhibitors to curb HCC cell proliferation[3].
体内研究
G007-LK exhibits an excellent pharmacokinetic profile in ICR mice[1].
G007-LK (100 mg/kg chow, pO.) significantly diminishes lineage tracing from LGR5+ intestinal stem cells in mice, specifically targeting LGR5+ WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50 mg/kg, pO.) also reduces canonical WNT signaling. Additionally, G007-LK (100 mg/kg chow, pO.) does not affect duodenal morphology[2].
体外研究
G007-LK effectively inhibits TNKS1 and TNKS2, with IC50 values of 46 nM and 25 nM, respectively, and demonstrates a cellular IC50 of 50 nM. It does not inhibit PARP1 at concentrations up to 20 μM and possesses a high IC50 value for CYP3A4 inhibition (>25 μM)[1].
G007-LK (0-20 μM) inhibits the growth of hepatocellular carcinoma (HCC) cells in a dose-dependent manner. It reduces YAP levels by increasing AMOTL1 and AMOTL2 in HCC cell lines. Moreover, G007-LK (0-20 μM) works in synergy with MEK and AKT inhibitors to curb HCC cell proliferation[3].
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