Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LW6 (HIF-1α inhibitor) 是一种新型 HIF-1抑制剂,IC50值为 4.4 μM。它降低 HIF-1α蛋白表达,但不影响 HIF-1β 表达。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 217 | 现货 | ||
2 mg | ¥ 313 | 现货 | ||
5 mg | ¥ 543 | 现货 | ||
10 mg | ¥ 758 | 现货 | ||
25 mg | ¥ 1,650 | 现货 | ||
50 mg | ¥ 2,990 | 现货 | ||
100 mg | ¥ 4,390 | 现货 | ||
500 mg | ¥ 9,490 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 582 | 现货 |
产品描述 | LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor. |
靶点活性 | MDH2:6.3 μM, HIF:4.4 μM |
体外活性 | LW6 decreases the expression of HIF-1α protein without affecting HIF-1β expression. LW6 affects the stability of the HIF-1α protein. LW6 promotes the degradation of wild type HIF-1α while 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. The knockdown of VHL does not abolish HIF-1α protein accumulation in the presence of LW6 which indicates that LW6 degraded HIF-1α via regulation of VHL expression[2]. 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[3]. LW6 inhibits the expression of HIF 1α induced by hypoxia in A549 cells at 20 mM, independently of the von Hippel Lindau protein. LW6 induces hypoxia selective apoptosis together with a reduction in the mitochondrial membrane potential[4]. |
体内活性 | LW6 demonstrates strong anti-tumor efficacy in vivo and causes a decrease in HIF-1α expression in frozen-tissue immunohistochemical staining in mice carrying xenografts of human colon cancer HCT116 cells[2]. |
细胞实验 | Inhibition of HIF-1a is assayed by a reporter assay using dualluciferase reporter assay system. HCT116 cells in 75-90% confluence are transiently co-transfected with pGL3-HRE-luciferase plasmid containing six copies of HREs from human VEGF genes and pRLSV40 encoding firefly renilla luciferase and incubated for 24 h. Cells are treated with LW6 or 17-AAG for 16 h before report assay. Luciferase activity is integrated over a 10 second period and measured using a luminometer[2]. |
别名 | HIF-1α inhibitor, CAY10585, LW8 |
分子量 | 435.51 |
分子式 | C26H29NO5 |
CAS No. | 934593-90-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (114.81 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2962 mL | 11.4808 mL | 22.9616 mL | 57.404 mL |
5 mM | 0.4592 mL | 2.2962 mL | 4.5923 mL | 11.4808 mL | |
10 mM | 0.2296 mL | 1.1481 mL | 2.2962 mL | 5.7404 mL | |
20 mM | 0.1148 mL | 0.574 mL | 1.1481 mL | 2.8702 mL | |
50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1481 mL | |
100 mM | 0.023 mL | 0.1148 mL | 0.2296 mL | 0.574 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LW6 934593-90-5 Angiogenesis Apoptosis Chromatin/Epigenetic Metabolism Dehydrogenase HIF/HIF Prolyl-Hydroxylase HIF LW 6 HIF-1α inhibitor Hypoxia-inducible factors inhibit CAY10585 HIF-PH CAY-10585 LW-6 HIFs LW 8 Inhibitor LW-8 HIF-1alpha inhibitor LW8 HIF-1a inhibitor CAY 10585 inhibitor