HPOB

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.target: HDAC6 [1]IC 50: 56nM [1]In vitro: HPOB causes growth inhibition of normal and transformed cells but does not induce cell death. HPOB enhances the effectiveness of DNA-damaging anticancer drugs in transformed cells but not normal cells. [1] Neuroprotective effect of HPOB demonstrated the crucial role of HDAC6 inhibition in reducing Cort-induced apoptosis in PC12 cells. Pre-treatment with HPOB remarkably reduces Cort-induced cytotoxicity and confirms the anti-apoptotic effect of HPOB via the caspase-3 activity assay and H33342/PI and TUNEL double staining. [2]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. [2]

Research Areas >> Cancer

HDAC6:0.056 μM (IC50)

HDAC3/NCOR2:1.7 μM (IC50)

HDAC8:2.8 μM (IC50)

HDAC1:2.9 μM (IC50)

HDAC10:3.0 μM (IC50)

HDAC2:4.4 μM (IC50)

[1]. Lee JH et al. 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.

[2]. Li ZY et al. HPOB, an HDAC6 inhibitor, attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway. Neurochem Int. 2016 Oct;99:239-51.

Trichostatin A | Entinostat (MS-275) | Romidepsin (FK228, Depsipeptide) | Mocetinostat(MGCD0103) | Ricolinostat (ACY-1215) | Sodium butyrate | RGFP 966 | Quisinostat | Tubacin | DL-Sulforaphane | CUDC-907 | LMK 235 | CI-994 | Tubastatin A | Sodium phenylbutyrate