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Synonyms | IBT 13131 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H16N2OS |
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分子量 | 308.40 | CAS No. | 313553-47-8 | ||||
Solubility (25°C)* | 体外 | DMSO | 61 mg/mL (197.79 mM) | ||||
Ethanol | 61 mg/mL (197.79 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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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. |
製品説明 | INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction. |
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in vitro | INH1 reduces the association of Hec1 with kinetochore and decreases global Nek2 protein level in cells. INH1 effectively inhibits the proliferation of human breast cancer lines with GI50 of 10-21 μM. Moreover, INH1 also elicits cell killing activity in part through impairing the Hec1/Nek2 pathway for the spindle checkpoint regulation. [1] |
in vivo | INH1 (100 mg/kg i.p.) inhibits breast tumor growth in mice bearing MDA-MB-468 human breast cancer xenograft. [1] |
キナーゼアッセイ | Binding assays | |
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Surface plasma resonance (SPR) assays are performed at 22.5°C in HBSD buffer [10 mmol/L HEPES, 150 mmol/L NaCl, 0.1% DMSO (pH 7.5)] on Biacore 3000. 6×His-Hec1 and GST-Nek2 are purified. NTA sensor chip or glutathione-modified CM5 chip are used to capture His-Hec1 and GST-Nek2, respectively. The capture level is about 140 to 180 resonance units (RU) at the flow rate of 5 μL/min. For the binding assay, chips are sequentially treated with compounds (1 or 20 μmol/L) and then proteins (50 μg/mL). Retained RUs are recorded and processed (triplicate experiments). | ||
細胞アッセイ | 細胞株 | MDA-MB-468, SKBR3, T47D, MDA-MB-361, ZR-75-1, HBL100, MDA-MB-435, HS578T, and MCF10A cells. |
濃度 | ~50 μM | |
反応時間 | 3 days | |
実験の流れ | Standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays with a 3-d drug treatment procedure are performed to measure the dose-dependent cytotoxicity of INH1 in cultured cells. Triplicate sets are measured and compiled for final data presentation. | |
動物実験 | 動物モデル | Athymic female BALB/c nude mice bearing MDA-MB-468 human breast cancer xenografts. |
投薬量 | ~100 mg/kg | |
投与方法 | i.p. |
Destabilizing NEK2 overcomes resistance to proteasome inhibition in multiple myeloma [ J Clin Invest, 2018, 128(7):2877-2893] | PubMed: 29863498 |
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。