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- 2025年12月05日
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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：
HIF-1α inhibitor; LW8
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥726.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥264.0 |
| 规格： | 5 mg | 产品价格： | ￥660.0 |
| 规格： | 10 mg | 产品价格： | ￥920.0 |
| 规格： | 25 mg | 产品价格： | ￥2000.0 |
| 规格： | 50 mg | 产品价格： | ￥3800.0 |
| 规格： | 100 mg | 产品价格： | ￥5700.0 |
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LW6
CAS No. : 934593-90-5
MCE 国际站：LW6
产品活性：LW6 (HIF-1α inhibitor) 是新颖的 HIF-1 抑制剂，IC50 值为 4.4 μM。LW6 降低 HIF-1α 蛋白表达，而不影响 HIF-1β 表达。
研究领域：Metabolic Enzyme/Protease | Apoptosis
作用靶点：HIF/HIF Prolyl-Hydroxylase | Apoptosis
In Vitro: LW6 affects the stability of the HIF-1α protein. LW6 promotes the degradation of wild type HIF-1α, but not of a DM-HIF-1α with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain. LW6 induces the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1α for proteasomal degradation. In the presence of LW6, knockdown of VHL does not abolish HIF-1α protein accumulation, indicating that LW6 degraded HIF-1α via regulation of VHL expression. In MDCKII-BCRP cells overexpressing BCRP, LW6 enhances significantly the cellular accumulation of mitoxantrone, a BCRP substrate. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 µM. LW6 inhibits the expression of HIF 1α induced by hypoxia in A549 cells at 20 µM, independently of the von Hippel Lindau protein. LW6 induces hypoxia selective apoptosis together with a reduction in the mitochondrial membrane potential.
In Vivo: In mice carrying xenografts of human colon cancer HCT116 cells, LW6 demonstrates strong anti-tumor efficacy in vivo and causes a decrease in HIF-1α expression in frozen-tissue immunohistochemical staining.
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