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HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs. In HFS cells, HPOB enhances transformed cell death induced by etoposide, doxorubicin, or SAHA. HPOB also enhancing etoposide-induced transformed cell death via the apoptotic pathway in transformed cells.
In vivo, on corticosterone (Cort)-induced apoptosis and explors the possible mechanism of action of HPOB in rat adrenal pheochromocytoma (PC12) cells, which possesses typical neuron features and expresses high levels of glucocorticoid receptors. In mice bearing CWR22 human prostate cancer xenografts, HPOB (300 mg/kg/d i.p.), when in combination with SAHA, causes suppression of the growth of established tumors, while produces no significant suppression when used alone.
| Cell Experiment | |
|---|---|
| Cell lines | HFS, A549, LNCaP, and U87 cells |
| Preparation method | Normal (HFS) and transformed (LNCaP, A549, and U87) cells are cultured with indicated doses of HPOB for 72 h. Five micromolars SAHA is a positive control.Graphs were constructed using Prism 5. |
| Concentrations | ~32 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing CWR22 human prostate cancer xenografts |
| Formulation | DMSO |
| Dosages | 300 mg/kg daily |
| Administration | i.p. |
| Molecular Weight | 314.34 |
| Formula | C17H18N2O4 |
| CAS Number | 1429651-50-2 |
| Solubility (25°C) | DMSO: ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
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| Givinostat hydrochloride monohydrate
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor. The IC50 values for maize HDAC preparations HD2, HD-1B and HD-1A are 10, 7.5 and 16 nM respectively. |
| Niltubacin
Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. |
| Tubacin
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. |
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