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LW6

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。

CAS号

934593-90-5

分子式

C26H29NO5

主要靶点

Apoptosis|HIF|Dehydrogenase|HIF/HIF Prolyl-Hydroxylase

仅限科研使用

Cat No : CM04469

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Synonyms

LW8|CAY10585|HIF-1α inhibitor

验证数据展示

  • CAS No.: 934593-90-5

    LW6
    CAS#: 934593-90-5

产品信息

LW6 is a novel HIF-1 inhibitor.

CAS号 934593-90-5
分子式 C26H29NO5
主要靶点 Apoptosis|HIF|Dehydrogenase|HIF/HIF Prolyl-Hydroxylase
主要通路 表观遗传|代谢|凋亡|血管生成
分子量 435.52
纯度 99.10%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LW8|CAY10585|HIF-1α inhibitor

靶点活性

MDH2:6.3 μM|HIF:4.4 μM

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].

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].

溶解度

DMSO:33 mg/mL

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].

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

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