HPOB 是一种高效、选择性的 HDAC6 抑制剂，IC50 为 56 nM。 HPOB 对其他 HDAC 的效力降低了 30 倍以上。 HPOB 可增强 DNA 破坏性抗癌剂在转化细胞而非正常细胞中的有效性。 HPOB 不会阻断 HDAC6 的泛素结合活性。
| Cas No. |
1429651-50-2 |
| 化学名 |
N-hydroxy-4-(2-((2-hydroxyethyl)(phenyl)amino)-2-oxoethyl)benzamide |
| Canonical SMILES |
OCCN(C(CC1=CC=C(C(NO)=O)C=C1)=O)C2=CC=CC=C2 |
| 分子式 |
C17H18N2O4 |
| 分子量 |
314.34 |
| 溶解度 |
≥ 31.4mg/mL in DMSO |
| 储存条件 |
Store at -20℃ |
| General tips |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition |
Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 半岛bd体育手机客户端 描述 |
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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