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LW6

LW6

产品编号 T3494   CAS 934593-90-5
别名: HIF-1α inhibitor, LW8, CAY10585

LW6 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。

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LW6, CAS 934593-90-5
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产品目录号及名称: LW6 (T3494)
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纯度: 99.10%
纯度: 98.1%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LW6 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, LW8, CAY10585
分子量 435.52
分子式 C26H29NO5
CAS No. 934593-90-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 33 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Naik R , Won M , Ban H S , et al. Synthesis and Structure–Activity Relationship Study of Chemical Probes as Hypoxia Induced Factor-1α/Malate Dehydrogenase 2 Inhibitors[J]. Journal of Medicinal Chemistry, 2014, 57(22):9522-9538. 2. Lee K, et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9. 3. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein. 4. Sato M, et al. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells. Mol Med Rep. 2015 Sep;12(3):3462-8. 5. Zhu B, Wu Y, Huang S, et al. Uncoupling of macrophage inflammation from self-renewal modulates host recovery from respiratory viral infection[J]. Immunity. 2021

文献引用

1. Zhu B, Wu Y, Huang S, et al. Uncoupling of macrophage inflammation from self-renewal modulates host recovery from respiratory viral infection. Immunity. 2021, 54(6): 1200-1218. e9.
HIF-2α agonist 2 Izilendustat Panaxadiol Tilorone dihydrochloride IOX2 Notoginsenoside Ft1 Chloramphenicol Glucosamine

相关化合物库

该产品包含在如下化合物库中:
抗胰腺癌化合物库 NO PAINS 化合物库 经典已知活性库 糖代谢化合物库 细胞凋亡化合物库 抗衰老化合物库 血管生成库 细胞重编程化合物库 干细胞分化化合物库 抗癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

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技术支持

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。

Keywords

LW6 934593-90-5 Angiogenesis Apoptosis Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase Dehydrogenase HIF LW 6 LW-8 Hypoxia-inducible factors inhibit HIF-PH HIF-1α inhibitor LW8 CAY10585 LW-6 HIFs Inhibitor LW 8 inhibitor

 

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