| 名称 | G007-LK |
| 描述 | G007-LK is a selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively. |
| 细胞实验 | Cell lines: APC-mutant CRC cell lines COLO-320DM. Concentrations: ~0.2 μM. Method: For colony formation assays,cells are seeded at 500 cells/well in 2 mL medium.Cell line in triplicate wells is treated with either 0.06% DMSO or compound in 0.06% DMSO and incubated for up to 17 days or until colonies became sufficiently large to quantify.Colonies are stained with 200 μL of 12 mM 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide to each well for 1 h,and colony numbers are quantitated with a GelCount scanner at 1200 dpi resolution. |
| 激酶实验 | TNKS1 and TNKS2 in vitro biochemical assays: G007-LK inhibitory activity at various doses (duplicates) is tested twice by TNKS1, TNSK2 Chemiluminescent Assay Kits, and the luminescence is measured. |
| 动物实验 | Animal Models: Human APC –mutant CRC xenograft COLO-320DM. Formulation: 15% DMSO,17.5% Cremophor EL,8.75% ethanol,8.75% Miglyol 810N,50% PBS. Dosages: 20 mg/kg. Administration: intraperitoneal injection twice daily |
| 体外活性 | G007-LK在异种移植和基因工程CRC模型中显示出抗肿瘤效力.在COLO-320DM模型中,G007-LK降低了tankyrases 1和tankyrases 2蛋白水平,稳定了AXIN1和AXIN2,并降低了β-catenin水平.G007-LK治疗增加COLO-320DM肿瘤中KRT20和TM4SF4的表达. G007-LK（20 mg/kg每日两次）达到61％的肿瘤生长抑制.G007-LK降低正常肠道中的Wnt/β-连环蛋白信号传导和细胞增殖. |
| 体内活性 | G007-LK通过防止多聚（ADP-核糖基）依赖性的AXIN降解来降低Wnt /β-连环蛋白信号传导,由此促进β-连环蛋白去稳定化。G007-LK在细胞培养中完全阻断配体驱动的Wnt/β-连环蛋白信号传导,并在大多数CRC细胞系中显示对约50％APC突变驱动的信号传导的抑制。 G007-LK（0.2 μM）将有丝分裂中的COLO-320DM细胞数量从24％降低至12％,并将S期中的HCT-15细胞从28％降低至18％。G007-LK抑制CRC系列COLO-320DM和SW403中的集落形成。 G007-LK抑制器官生长,IC50为80 nM。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Corn Oil : 3.3 mg/mL (6.23 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (175.48 mM), Sonication is recommended.
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| 关键字 | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | TNKS2 | TNKS1 | poly ADP ribose polymerase | PARP | Inhibitor | inhibit | G007-LK | G-007-LK | G007LK | G007 LK | beta-catenin | betacatenin | bcatenin |
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