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HPOB

Catalog No.GC11574

HPOB est un inhibiteur très puissant et sélectif de HDAC6 avec une IC50 de 56 nM. HPOB affiche > 30 fois moins puissant contre les autres HDAC. HPOB améliore l'efficacité des agents anticancéreux endommageant l'ADN dans les cellules transformées, mais pas dans les cellules normales. HPOB ne bloque pas l'activité de liaison À l'ubiquitine de HDAC6.

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HPOB Chemical Structure

Cas No.: 1429651-50-2

Taille Prix Stock Qté
5mg
46,00 $US
En stock
10mg
74,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56nM, >30 fold less potent against other HDACs. [1]
HDAC6 is one of the eleven human zinc-dependent HDACs with two catalytic domains and one ubiquitin-binding domain at the C-terminal. It exhibits various biological functions including regulation of microtubule dynamics and degradation of misfolded proteins. It involves in many cellular pathways related to normal and tumor cell growth, migration and death. [1]
In normal HFS and transformed LNCaP cells, HPOB inhibited cell growth but not viability, induced acetylation of α-Tubulin, but not histones. HPOB enhanced etoposide-, doxorubicin-, and SAHA-induced cell death in transformed cell but not in normal cell. HPOB enhanced the effectives of anticancer drugs via apoptotic pathway and activated DNA damage response in transformed cell. [1]
HPOB is well-tolerated in mice carrying human prostate cancer CWR22 xenograft and enhances cytotoxicity effects of anticancer drug SAHA in these animals. [1]
References:
1.  Lee JH, Mahendran A, Yao Y, Ngo L, Venta-Perez G, Choy ML, Kim N, Ham WS, Breslow R, Marks PA. Development of a histone deacetylase 6 inhibitor and its
biological effects. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9.

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