HPOB |
Catalog No.GC11574 |
HPOB es un inhibidor altamente potente y selectivo de HDAC6 con un IC50 de 56 nM. HPOB muestra >30 veces menos potente que otros HDAC. HPOB mejora la eficacia de los agentes anticancerÍgenos que daÑan el ADN en las células transformadas, pero no en las células normales. HPOB no bloquea la actividad de uniÓn a ubiquitina de HDAC6.
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Cas No.: 1429651-50-2
Sample solution is provided at 25 µL, 10mM.
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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