| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408536-1ml |
1ml |
现货  |
|
| 英文别名 | 1-(4-methoxybenzyl)-N-hydroxy-1H-indole-6-carboxamide |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | PCI-34051 |
| 生化机理 | PCI-34051 是一种强效特异性 HDAC8 抑制剂，在无细胞试验中的 IC50 为 10 nM。它对 HDAC1 和 6 的选择性超过 200 倍，对 HDAC2、3 和 10 的选择性超过 1000 倍。PCI-34051 可诱导依赖于 Caspase 的细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
PCI-34051是一种有效的，特异性的HDAC8抑制剂，无细胞试验中IC50为10 nM。比作用于HDAC1和6选择性高200多倍，比作用于HDAC2， 3，和10选择性高1000倍。A potent and specific HDAC8 inhibitor. Information PCI-34051 is a potent and specificHDAC8inhibitor withIC50of 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. PCI-34051 induces caspase-dependentapoptosis. PCI-34051 possesses promising potency for HDAC8 with a Ki 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. In vivo
cell lines： Concentrations：5 μM Incubation Time：24 hours Powder Purity:≥97% |
| IC50 | HDAC8, IC50: 10 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC=C(C[N]2C=CC3=C2C=C(C=C3)C(=O)NO)C=C1 |
| 分子量 | 296.32 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 38 mg/mL (195.69 mM); |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
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