化合物LW6 T3494

Product Introduction
Bioactivity


英文名: LW6

描述: 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。

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].

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].

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

溶解度: DMSO : 50 mg/mL (114.81 mM)


关键字: LW 6 | Apoptosis | Hypoxia-inducible factors | inhibit | HIF-PH | HIF/HIF Prolyl-Hydroxylase | CAY-10585 | LW6 | LW-6 | HIFs | LW 8 | Inhibitor | LW-8 | HIF-1alpha inhibitor | HIF-1a inhibitor | CAY 10585

相关产品: MK-886 | Mepazine | Cucurbitacin IIb | BI-6C9 | Simmiparib | Verbascoside | Antitumor agent-103 | 3-Dehydrotrametenolic acid | Cucurbitacin B | CMLD-2

相关库: HIF-1 Signaling Pathway Compound Library | Glycometabolism Compound Library | Transcription Factor-Targeted Compound Library | Anti-Cancer Metabolism Compound Library | Glutamine Metabolism Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途