Aminoxyrone (AX)

Chemical Structure : Aminoxyrone

Catalog No.: PC-63505Not For Human Use, Lab Use Only.

Aminoxyrone (AX) is a novel peptidometic C-terminal HSP90 inhibitor by targeting HSP90 dimerization via the C-terminal domain (CTD) with Kd of 27.4 uM.

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Biological Activity

Aminoxyrone (AX) is a novel peptidometic C-terminal HSP90 inhibitor by targeting HSP90 dimerization via the C-terminal domain (CTD) with Kd of 27.4 uM.
Aminoxyrone 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.
Aminoxyrone triggers the degradation of HSP90 client proteins without elevating the expression of HSPs (HSP70, HSP40 & HSP27).
Aminoxyrone 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.

Physicochemical Properties

M.Wt	994.153
Formula	C50H71N7O14
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

References

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

Aminoxyrone (AX)

Biological Activity

Physicochemical Properties

References

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