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- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1380672-07-0
- 规格:
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1399.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1200.0 |
| 规格: | 10 mg | 产品价格: | ¥2000.0 |
| 规格: | 25 mg | 产品价格: | ¥3800.0 |
| 规格: | 50 mg | 产品价格: | ¥5500.0 |
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G007-LK
CAS No. : 1380672-07-0
MCE 国际站:G007-LK
产品活性:G007-LK 是一种有效的,选择性的 TNKS1 和 TNKS2 抑制剂,IC50值分别为 46 nM 和 25 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:PARP
In Vitro: G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively, and a cellular IC50 of 50 nM. G007-LK shows no inhibition of PARP1 at doses up to 20 μM, and has a high CYP3A4 inhibition IC50 value (>25 μM). G007-LK (0-20 μM) dose-dependently inhibits hepatocellular carcinoma (HCC) cell growth. G007-LK also downregulates the levels of YAP by upregulating AMOTL1 and AMOTL2 in HCC cell lines. In addition, G007-LK (0-20 μM) synergizes with MEK and AKT inhibitors to suppress HCC cell proliferation.
In Vivo: G007-LK displays great pharmacokinetic profile in ICR mice. G007-LK (100 mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5+ intestinal stem cells in mice. G007-LK (100 mg/kg chow, p.o.) specifically targets LGR5+ WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50 mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000 mg/kg chow, p.o) shows no effect on the alteration of duodenal morphology.
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