PCI-34051

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PCI-34051 是一种有效且特异性的 HDAC8 抑制剂，IC50 为 10 nM。

PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10.

PCI-34051 inhibits pure recombinant HDAC8 with Ki of 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.

Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling.

PCI34051 | PCI 34051 | PCI-34051

Cell Cycle/DNA Damage

HDAC

HDAC1| HDAC10| HDAC2| HDAC6| HDAC8

Cancer

——

950762-95-5

296.32

C17H16N2O3

>98% (HPLC)

DMSO:59 mg/mL (199.1 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

O=C(C1=CC2=C(C=C1)C=CN2CC3=CC=C(OC)C=C3)NO

N-hydroxy-1-(4-methoxybenzyl)-1H-indole-6-carboxamide

(-20℃)

With Ice Pack

≥ 2 years