PCI-34051

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Chemical Structure| 950762-95-5 同义名 : -
CAS号 : 950762-95-5
货号 : A190192
分子式 : C17H16N2O3
纯度 : 99%+
分子量 : 296.32
MDL号 : MFCD11114393
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(101.24 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • HDAC8

    HDAC8, IC50:10 nM
描述 PCI-34051 is an inhibitor of pure recombinant HDAC8, exhibits a Ki of 10 nM, demonstrating >200-fold selectivity over other tested HDACs, including HDACs 1, 2, 3, 6, and 10. Derived from a low molecular weight hydroxamic acid scaffold, PCI-34051 initially possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to other class I HDACs. In cell lines derived from T-cell lymphomas, such as Jurkat and HuT78, PCI-34051 induces apoptosis at low micromolar concentrations, while doses as high as 20 μM have no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines [1].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human Huh7 cells Function assay 3 days Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50=1.8 μM 25490700
human Jurkat cells Growth inhibition assay 72 h Growth inhibition of human Jurkat cells incubated for 72 hrs by MTS assay, GI50=11 μM 23116147
human MT2 cells Growth inhibition assay 72 h Growth inhibition of human MT2 cells incubated for 72 hrs by MTS assay, GI50=15 μM 23116147
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.37mL

0.67mL

0.34mL

16.87mL

3.37mL

1.69mL

33.75mL

6.75mL

3.37mL
参考文献

[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.