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- CAS号:
218924-25-5
- 规格:
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格: | 1mg | 产品价格: | ¥190.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥386.0 |
| 规格: | 5mg | 产品价格: | ¥386.0 |
| 规格: | 10mg | 产品价格: | ¥557.0 |
| 规格: | 25mg | 产品价格: | ¥1024.0 |
| 规格: | 50mg | 产品价格: | ¥1536.0 |
| 规格: | 100mg | 产品价格: | ¥2304.0 |
| 规格: | 200mg | 产品价格: | ¥3464.0 |
Product Introduction
Bioactivity
| 名称 | KNK437 |
| 描述 | KNK437 (Heat Shock Protein Inhibitor I), a pan-HSP inhibitor, suppresses the synthesis of inducible HSPs(HSP105, HSP72, and HSP40). |
| 细胞实验 | Thermotolerance is induced by incubating cells with 300 μM sodium arsenite for 90 min. Cells are preincubated with or without 100 μM KNK437 for 1 h before the sodium arsenite treatment. After treatment of the cells with sodium arsenite, cells are washed once with PBS and incubated at 37℃ for 5 h with or without KNK437. The effects of KNK437 on acquired thermotolerance are tested by heating the cells at 45°C for the indicated time. The surviving fraction is calculated as the plating efficiency of the treated cells divided by the plating efficiency of untreated control cells.(Only for Reference) |
| 激酶实验 | Metabolic Labeling and Gel Electrophoresis: COLO 320DM cells (200,000) are injected into each well of 12-well plastic plates 2 days before incubation in the presence of KNK437 for 1 h before heat shock. The cells are then heat-shocked at 42°C for 90 min or kept at 37°C for the same length of time and incubated at 37°C for 2 h. For metabolic labeling, cells are washed with PBS without Ca2+ or Mg2+ and incubated for 1 h with 1.22 MBq of [35S]methionine in 250 μL of methionine-free DMEM supplemented with 10% dialyzed fetal bovine serum. After metabolic labeling, cells are washed twice with PBS and lysed in a buffer containing 1% NP40, 0.15 M NaCl, 50 mM Tris-HCl (pH 8.0), 5 mM EDTA, and protease inhibitors [0.2 mM 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride, 2 mM N-ethylmaleimide, 1 μg/mL pepstatin, and 1 μg/mL leupeptin]. After centrifugation at 12,000×g for 20 min, cell extracts containing equal amounts of trichloroacetic acid-insoluble radioactivity are analyzed by two-dimensional gel electrophoresis (the one-dimensional gel electrophoresis is a nonequilibrium pH gradient gel electrophoresis, and the two-dimensional gel electrophoresis is 10% SDS-PAGE). |
| 体内活性 | KNK437(200 mg/kg,i.p.)未展现出任何抗肿瘤效果,且不提升非耐受性肿瘤的热敏感性。同样剂量的KNK437能够以协同方式增强分次加热治疗的抗肿瘤效果。[3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Corn Oil : 1 mg/mL (4.08 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 19.6 mg/mL (79.92 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.96 mg/mL (7.99 mM), Suspension. 10% DMSO+90% Saline : < 1.96 mg/mL (7.99 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. |
| 关键字 | KNK-437 | KNK437 | KNK 437 | Inhibitor | inhibit | HSP72 | HSP40 | HSP105 | HSP | Heat shock proteins |
| 相关产品 | Mequinol | Isoxazole | 7-Aminocephalosporanic acid | Palmitic acid sodium | Tamoxifen Citrate | Elesclomol | Rifabutin | Palmitic acid | Benzbromarone | Ethoxyquin | Tamoxifen | Adezmapimod |
| 相关库 | Inhibitor Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Oxidation-Reduction Compound Library | Metabolism Compound Library | Cytoskeletal Signaling Pathway Compound Library | Preclinical Compound Library | Membrane Protein-targeted Compound Library | Covalent Inhibitor Library | Endoplasmic Reticulum Stress Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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