KNK437

製品コードS7750 バッチS775001

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H11NO4
分子量 245.23 CAS No. 218924-25-5
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 15 mg/mL (61.16 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 KNK437は、HSP105、HSP72、HSP40などの誘導性HSPの合成を阻害する、パンHSP阻害剤です。
in vitro KNK437 dose-dependently inhibits the acquisition of thermotolerance and the induction of various HSPs including HSP105, HSP70, and HSP40 in COLO 320DM (human colon carcinoma) cells. This compound and quercetin inhibits thermotolerance in a dose-dependent manner in PC-3 cells. It decreases heat-induced accumulation of Hsp70 mRNA and protein in PC-3 and LNCaP cells.
in vivo KNK437 (200 mg/kg, i.p.) shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors. The same dose of this compound enhances the antitumor effects of fractionated heat treatment in a synergistic manner.

プロトコル(参考用のみ)

キナーゼアッセイ 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).
細胞アッセイ 細胞株 COLO 320DM cells
濃度 100 μM
反応時間 1 h
実験の流れ 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 this compound. The effects of this chemical 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.
動物実験 動物モデル C3H/He mice
投薬量 200 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/10850441/
  • https://pubmed.ncbi.nlm.nih.gov/21204621/
  • https://pubmed.ncbi.nlm.nih.gov/11205912/

カスタマーフィードバック

Data from [Data independently produced by , , Br J Haematol, 2013, 161(5):667-76]

Data from [Data independently produced by , , ONCOLOGY REPORTS, 2012, 28:1953-1958.]

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：

A potential role for Giardia chaperone protein GdDnaJ in regulating Giardia proliferation and Giardiavirus replication [ Parasit Vectors, 2023, 16(1):168] PubMed: 37226181
Activation of the IL-1β/KLF2/HSPH1 pathway promotes STAT3 phosphorylation in alveolar macrophages during LPS-induced acute lung injury. [ Biosci Rep, 2020, 40(3)] PubMed: 32091104
Inhibition of related JAK/STAT pathways with molecular targeted drugs shows strong synergy with ruxolitinib in chronic myeloproliferative neoplasm. [Barrio S, et al. Br J Haematol, 2013, 161(5):667-76] PubMed: 23560534
Hyperthermia reduces migration of osteosarcoma by suppression of autocrine motility factor. [Nakajima K, et al. Oncol Rep, 2012, 28(6):1953-8] PubMed: 23027359

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。

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