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- 详细信息
- 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.
- 英文名:
CB839 derivative
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- 规格:
10 mM * 1 mL/5 mg/10 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1633.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥1200.0 |
| 规格: | 10 mg | 产品价格: | ¥1900.0 |
| 规格: | 50 mg | 产品价格: | ¥5500.0 |
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Glutaminase-IN-1
CAS No. : 2247127-79-1
MCE 国际站:Glutaminase-IN-1
产品活性:Glutaminase-IN-1 (CB839 derivative) 是CB839 的一个衍生物,是1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂,其IC50 值为1 nM。Glutaminase-IN-1 (CB839 derivative) 具有提高细胞摄取和抗肿瘤的活性。
研究领域:Metabolic Enzyme/Protease
作用靶点:Glutaminase
In Vitro: Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC50 values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839.
In Vivo: Glutaminase-IN-1(10 mg/kg, s.c.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing mice.
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