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CAS No.: 950762-95-5

PCI-34051 Catalog No. CSN16819

Synonyms: PCI-34051

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

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HDAC8

IC50:10nM
描述PCI-34051 possesses promising potency for HDAC8 with a K of 10 nM. PCI-34051 has high selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 reveals greater than 200-fold selectivity over HDAC1 and HDAC6, and greater than 1000-fold selectivity over HDAC2, HDAC3 and HDAC10. PCI-34051 inhibits ovarian tumor line OVCAR-3 with a GI50 of 6 μM and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 at concentrations less than 25 μM at 24 hours nor at earlier timepoints. PCI-34051 induces a selective cytotoxic effect in cell lines derived only from T-cell malignancies. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours, another hallmark of apoptosis, consistent with the higher levels of caspase activity at this timepoint. PCI-34051 does not stimulate Bid cleavage, a characteristic effect of the extrinsic apoptotic pathway. While P116 and J.RT3-T.5 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line reveals a marked decrease in the extent of PCI-34051-induced apoptosis. In addition, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Mice(i.p.): 0.5 mg/kg^[3], 3 mg/kg^[4]

给药途径
i.p.

动物研究
剂量	Mice(i.p.): 0.5 mg/kg^[3], 3 mg/kg^[4]
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3747 mL
- 16.8736 mL
- 33.7472 mL
- 5 mM
- 0.6749 mL
- 3.3747 mL
- 6.7494 mL
- 10 mM
- 0.3375 mL
- 1.6874 mL
- 3.3747 mL

技术信息

CAS号

950762-95-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H16N2O3

运输

蓝冰

分子量

296.32

别名

PCI-34051

溶解度

DMSO	59.0 mg/mL (199.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+40%PEG300+5% tween80+50% water

5 mg/mL

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