| 产品编号 |
D51687 |
| 英文名称 |
LW 6
|
| 中文名称 |
|
| 别 名 |
methyl 3-[[2-[4-(2-adamantyl)phenoxy]acetyl]amino]-4-hydroxybenzoate; Hypoxia Inducible Factor-1alpha Inhibitor;
methyl 4-hydroxy-3-({[4-(tricyclo[3.3.1.1]dec-1-yl)phenoxy]acetyl}amino)benzoate;
Benzoic acid, 4-hydroxy-3-[[2-(4-tricyclo[3.3.1.1]dec-1-ylphenoxy)acetyl]amino]-, methyl ester;
Methyl 3-[({4-[(3s,5s,7s)-adamantan-1-yl]phenoxy}acetyl)amino]-4-hydroxybenzoate;
Methyl 3-({[4-(adamantan-1-yl)phenoxy]acetyl}amino)-4-hydroxybenzoate;
CAY10585; HIF-1α inhibitor; 3-[[[4-(金刚烷-1-基)苯氧基]乙酰基]氨基]-4-羟基苯甲酸甲酯；HIF-1α抑制剂； |
| 克 隆 号 |
|
| CAS |
934593-90-5 |
| 理论分子量 |
435.51 kDa |
| 检测分子量 |
|
| 性 状 |
Lyophilized |
| 保存条件 |
Store in dry, dark place for one year. |
| 注意事项 |
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications. |
| 产品介绍 |
LW6, was first identified and reported by a group scientists from Korea. LW8 was found to inhibits the accumulation of HIF-1alpha. LW6 decreased HIF-1alpha protein expression without affecting HIF-1beta expression. It was further found that LW8 promoted the degradation of wild type HIF-1alpha, but not of a DM-HIF-1alpha with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain (ODDD). LW6 did not affect the activity of prolyl hydroxylase (PHD), but induced the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1alpha for proteasomal degradation. In the presence of LW8, knockdown of VHL did not abolish HIF-1alpha protein accumulation, indicating that LW8 degraded HIF-1alpha via regulation of VHL expression. In mice carrying xenografts of human colon cancer HCT116 cells, LW8 demonstrated strong anti-tumor efficacy in vivo and caused a decrease in HIF-1alpha expression in frozen-tissue immunohistochemical staining. These data suggest that LW8 may be valuable in the development of a HIF-1alpha inhibitor for cancer treatment. (source: Biochem Pharmacol. 2010 Oct 1;80(7):982-9.)
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