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Chemical Structure : Aminoxyrone
Catalog No.: PC-63505Not For Human Use, Lab Use Only.
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.
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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.
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.
| M.Wt | 994.153 | |
| Formula | C50H71N7O14 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bhatia S, et al. Blood. 2018 May 3. pii: blood-2017-10-810986.
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