Aminoxyrone ( —— )

产品货号. M17004 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

Aminoxyrone
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

Aminoxyrone 是一种新型肽组学 C 端 HSP90 抑制剂，通过 C 端结构域 (CTD) 靶向 HSP90 二聚化，Kd 为 27.4 uM。
产品描述

Aminoxyrone is a novel peptidometic C-terminal HSP90 inhibitor by targeting HSP90 dimerization via the C-terminal domain (CTD) with Kd of 27.4 uM; destabilizes BCR-ABL1 without inducing HSR in vitro and in vivo, additionally reduces pAKT-S473, pS6 expression and expression of client proteins associated with HSP90 chaperone activity, involving t-AKT, t-STAT5a, t-CRKL, cMYC, and BCL2; triggers the degradation of HSP90 client proteins without elevating the expression of HSPs (HSP70, HSP40 & HSP27); significantly inhibits cell growth and induces apoptosis of human leukemic stem cells (LSCs) with average EC50 of 20.94 uM, Aminoxyrone is effective in imatinib resistant CML and lacks heat shock response.
体外实验

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体内实验

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同义词

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通路

Cytoskeleton/Cell Adhesion Molecules
靶点

HSP
受体

HSP
研究领域

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适应症

——

CAS Number

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分子量

994.153
分子式

C50H71N7O14
纯度

>98% (HPLC)
溶解度

——
SMILES

——
化学全称

benzyl (((2R,6R,10R,14R,18R,22R)-6-benzyl-10,14-di((S)-sec-butyl)-22-carbamoyl-18-isobutyl-24-methyl-3,7,11,15,19-pentaoxo-1-phenyl-5,9,13,17,21-pentaoxa-4,8,12,16,20-pentaazapentacosan-2-yl)oxy)carbamate

1. Bhatia S, et al. Blood. 2018 May 3. pii: blood-2017-10-810986.

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