Aminoxyrone( —— )

Catalog No. M17004 CAS No. ——

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

Aminoxyrone
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

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In Vivo

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Synonyms

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Pathway

Cytoskeleton/Cell Adhesion Molecules
Target

HSP
Recptor

HSP
Research Area

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Indication

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CAS Number

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Formula Weight

994.153
Molecular Formula

C50H71N7O14
Purity

>98% (HPLC)
Solubility

——
SMILES

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Chemical Name

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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