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LW6

LW6

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

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。

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LW6 Chemical Structure
LW6, CAS 934593-90-5
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
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 (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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (114.81 mM)

溶液配制表

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

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TargetMol Library Books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

TargetMol Library Books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.
MPI-0479605 Enpp/Carbonic anhydrase-IN-2 Neobavaisoflavone VAS 3947 ZINC69391 Pexidartinib Ethoxysanguinarine Corilagin

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌细胞代谢库 抗胰腺癌化合物库 表观遗传库 已知活性化合物库 糖代谢化合物库 抗代谢疾病化合物库 代谢化合物库 经典已知活性库 HIF-1化合物库

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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。

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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 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

 

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