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受注：045-509-1970 |
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化学情報
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Synonyms | AC1-001 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C26H29NO5 |
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| 分子量 | 435.51 | CAS No. | 934593-90-5 | |
| Solubility (25°C)* | 体外 | DMSO | 13 mg/mL (29.85 mM) | |
| Ethanol | 1 mg/mL (2.29 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | CAY10585 (LW 6) is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays. |
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| in vitro | LW6 inhibits HIF-1α expression induced by hypoxia. It promotes apoptosis preferentially in hypoxic cells. Treatment with LW6 presents no additive effect on cell cycle arrest. LW6 induces ROS formation through the depolarization of MMP in hypoxic cells. Although LW6 increases mitochondrial ROS production, the combination with hypoxia induces a marked increase in ROS production and this high level is maintained up until 24 h. LW6 is also a specific inhibitor of MDH2. As MDH2 is known to serve a significant role in the citric acid cycle at the mitochondrial membrane, LW6 indirectly reduces the activity of the mitochondrial respiratory chain through the inhibition of MDH2[1]. In MDCKII-BCRP cells overexpressing BCRP, LW6 enhances significantly (p < 0.05) the cellular accumulation of mitoxantrone, a BCRP substrate, and is more potent than Ko143, a well-known BCRP inhibitor. In contrast to BCRP, LW6 has no inhibition effect on the functional activity and gene expression of P-gp[2]. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 μM. Furthermore, cells become more susceptible to the cytotoxicity of anticancer drugs in the presence of LW6[3]. |
| in vivo | LW6 exerts marked anti-tumor efficacy in vivo and causes reductions in HIF-1α expression levels in mice carrying xeno-grafts of HCT116 cells[1]. LW6 improves the cytotoxicity and bioavailability of anticancer drugs translocated by BCRP[3]. |
プロトコル(参考用のみ)
| 細胞アッセイ | 細胞株 | A549 cells |
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| 濃度 | 5-100 μM | |
| 反応時間 | 24 h | |
| 実験の流れ | Cells are incubated in 96-well ELISA Plates with 100 μl culture medium at 2×105 cells/ml with or without LW6 for 24 h. Cell viability is assessed by the dimethyl thiazolcarboxy-methoxyphenylsulfophenyltetrazolium (MTS) assay. The absorbance is measured at 490 and 620 nm using a microplate reader. For the trypan blue dye. exclusion test, cells are stained by phosphate-buffered saline (PBS) containing 0.1% trypan blue. Cell viability is assessed by counting the number of unstained cells. |
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| 動物実験 | 動物モデル | Male Sprague-Dawley rats |
| 投薬量 | 10 mg/kg | |
| 投与方法 | p.o. |
参考
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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| WNT-inhibitory factor 1-mediated glycolysis protects photoreceptor cells in diabetic retinopathy [ J Transl Med, 2024, 22(1):245] | PubMed: 38448948 |
| Commensal microbiome promotes hair follicle regeneration by inducing keratinocyte HIF-1α signaling and glutamine metabolism [ Sci Adv, 2023, 9(1):eabo7555] | PubMed: 36598999 |
| IL-17 Induces Autophagy Dysfunction to Promote Inflammatory Cell Death and Fibrosis in Keloid Fibroblasts via the STAT3 and HIF-1α Dependent Signaling Pathways [ Front Immunol, 2022, 13:888719] | PubMed: 35757697 |
| Downregulation of miR-491-5p promotes neovascularization after traumatic brain injury [ Neural Regen Res, 2022, 17(3):577-586] | PubMed: 34380897 |
| Effects and mechanisms of 6-hydroxykaempferol 3,6-di-O-glucoside-7-O-glucuronide from Safflower on endothelial injury in vitro and on thrombosis in vivo [ Front Pharmacol, 2022, 13:974216] | PubMed: 36210813 |
| The PER1/HIF-1alpha negative feedback loop promotes ferroptosis and inhibits tumor progression in oral squamous cell carcinoma [ Transl Oncol, 2022, 18:101360] | PubMed: 35134674 |
| Differentiated embryo chondrocyte 1, induced by hypoxia-inducible factor 1α, promotes cell migration in oral squamous cell carcinoma cell lines [ Oral Surg Oral Med Oral Pathol Oral Radiol, 2022, 133(2):199-206] | PubMed: 34758939 |
| RASA4 inhibits the HIFα signalling pathway to suppress proliferation of cervical cancer cells [ Bioengineered, 2021, 10.1080/21655979.2021.2002499] | PubMed: 34752201 |
| FGFR3 deficiency enhances CXCL12-dependent chemotaxis of macrophages via upregulating CXCR7 and aggravates joint destruction in mice [ Ann Rheum Dis, 2020, 79(1):112-122] | PubMed: 31662319 |
| MicroRNA-137 exerts protective effects on hypoxia-induced cell injury by inhibiting autophagy/mitophagy and maintaining mitochondrial function in breast cancer stem-like cells [ Oncol Rep, 2020, 44(4):1627-1637] | PubMed: 32945512 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。