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. |
溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 12 mg/mL (48.9 mM)
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关键字 | HSP | KNK-437 | inhibit | Heat shock proteins | KNK437 | KNK 437 | Inhibitor |
相关产品 | SNX2112 | Teprenone | SNX0723 | Gedunin | Tamoxifen Citrate | Rifabutin | Paeoniflorin | Tamoxifen | Ethoxyquin | Ganetespib | DN401 | KRIBB11 |
相关库 | 抑制剂库 | 抗乳腺癌化合物库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌化合物库 | 已知活性化合物库 | 氧化还原化合物库 | 临床前化合物库 | 共价抑制剂库 | 内质网应激化合物库 |