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CAS No.: 218924-25-5

KNK437/KNK 437(热激蛋白抑制剂I) Catalog No. CSN17321

Synonyms: Heat Shock Protein Inhibitor I;Hsp Inhibitor I

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

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实验方案

技术信息

生物活性

描述HSPs (heat shock proteins) can be transiently synthesized when the cells exposure to heat or other stress, such as sodium arsenite, heavy metals, or amino acid analogues. Especially, a number of HSPs, including HSP40, HSP47, HSP70, HSP90, and HSP100 can be enhanced by heat shock and regulated at the transcriptional level in mammalian cells. KNK437 is an inhibitor of the acquisition of thermotolerance, which can inhibit various HSPs at the mRNA level transiently during the heat shock. Pre-treatment with 25-200μM KNK437 before the first heat treatment could dose-dependently inhibit the acquisition of thermotolerance of COLO 320DM or HeLa S3 cells by heat shock. Similarly, the inhibition of the acquisition of thermotolerance by 300μM sodium arsenite can be achieved by 100μM KNK437 pre-treatment in COLO 320DM cells. Addition of 100μM KNK437 during heat shock could specially inhibited the induction of major HSPs, including HSP110, HSP105, HSP72 and HSP40, but not the constitutively expressed HSP family proteins HSC73 or HSP90, in COLO 320DM. Treatment with KNK437 alone without heat shock did not show cytotoxicity^[1]. Administration intraperitoneally of KNK473 at dose of 200mg/kg did not affect the tumor growth in mice, but dose at 6h prior to the first treatment can enhance the antitumor effects of fractionated heat treatment at 44°C in a synergistic manner, accompanied with inhibition of HSP72 observed in vivo^[2].
动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.), 62.5 mg/kg - 500 mg/kg^[2] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.), 62.5 mg/kg - 500 mg/kg^[2] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0778 mL
- 20.3890 mL
- 40.7779 mL
- 5 mM
- 0.8156 mL
- 4.0778 mL
- 8.1556 mL
- 10 mM
- 0.4078 mL
- 2.0389 mL
- 4.0778 mL

技术信息

CAS号

218924-25-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H11NO4

运输

蓝冰

分子量

245.23

别名

Heat Shock Protein Inhibitor I;Hsp Inhibitor I

溶解度

DMSO	15.0 mg/mL (61.2 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+corn oil

2 mg/mL

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KNK437/KNK 437(热激蛋白抑制剂I) Catalog No. CSN17321

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