化合物KNK437 T2444

Product Introduction
Bioactivity


英文名: KNK437

描述: KNK437 (Heat Shock Protein Inhibitor I) 是一种 HSP 抑制剂，抑制 HSP40，HSP70 和 HSP105 的活化。

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 12 mg/mL (48.9 mM)


关键字: HSP | KNK-437 | inhibit | Heat shock proteins | KNK437 | KNK 437 | Inhibitor

相关产品: NPX800 | Elesclomol | VER-82576 | HSP90-IN-23 | Col003 | Pimitespib | Ethoxyquin | HSP90-IN-25 | Eupalinolide A | HSP27 inhibitor J2

相关库: Anti-Cancer Compound Library | Anti-Metabolism Disease Compound Library | Endoplasmic Reticulum Stress Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | Preclinical Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library | Bioactive 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