"目录号: HY-15224
Cell Cycle/DNA DamageEpigenetics-
PCI-34051 是一种有效的选择性的HDAC8抑制剂，IC50为 10 nM。
HDAC
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生物活性
Description
PCI-34051 is a potent and selectiveHDAC8inhibitor withIC50of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
IC50& Target
IC50: 10 nM (HDAC8), 2.9 μM (HDAC6), 4 μM (HDAC1), 13 μM (HDAC10)[1]
In Vitro
PCI-34051 inhibits pure recombinant HDAC8 with Kiof 10 nM with >200-fold selectivity over the other HDACs tested, including HDACs 1, 2, 3, 6 and 10. PCI-34051 is derived from a low molecular weight hydroxamic acid scaffold that possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs. PCI-34051 is found to induce apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, whereas doses as high as 20 μM has no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines[1].
In Vivo
Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling[2].
References
[1].Balasubramanian S, et al. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia. 2008 May;22(5):1026-34.
[2].Ren Y, et al. Therapeutic effects of histone deacetylase inhibitors in a murine asthma model. Inflamm Res. 2016 Dec;65(12):995-1008.