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KX1-004
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KX1-004图片
CAS NO:518058-84-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
KX1-004 是一种有效的、非 ATP 竞争性的 Src-PTK 抑制剂,IC50 为 40 μM。
Cas No.518058-84-9
化学名5-fluoro-N-(3-hydroxybenzyl)-1H-indole-2-carboxamide
Canonical SMILESFC1=CC(C=C(C(NCC2=CC=CC(O)=C2)=O)N3)=C3C=C1
分子式C16H13FN2O2
分子量284.29
溶解度≥ 10.1mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

KX1-004 is a non-ATP competitive inhibitor of pp60c-src with IC50 value of 40 μM [1].

KX1-004 is a close analog of the indole-based Src-PTK inhibitors reported previously. It has a 5-fluoro group and showed potent inhibition activity in isolated Src-PTK assay. KX1-004 was found to have protective effect in noise-induced hearing loss. The chinchillas treated with 30 μM KX1-004 were exposed to continuous noise. And the results showed that treated ears exhibited up to 40 dB less threshold shift (TTS) and up to 25 dB less permanent threshold shift (PTS) than control ears. KX1-004 treatment also significantly reduced outer hair cell (OHC) loss than control. Besides that, KX1-004 was proved to reduce the hearing loss and hair cell loss associated with impulse noise exposure markedly [1, 2].

References:
[1] Harris K C, Hu B, Hangauer D, et al. Prevention of noise-induced hearing loss with Src-PTK inhibitors. Hearing research, 2005, 208(1): 14-25.
[2] Milkiewicz K L, Marsilje T H, Woodworth Jr R P, et al. The design, synthesis and activity of non-ATP competitive inhibitors of pp60 c-src tyrosine kinase. Part 2: Hydroxyindole derivatives. Bioorganic & medicinal chemistry letters, 2000, 10(5): 483-486.