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Droxinostat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Droxinostat图片
CAS NO:99873-43-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
NS 41080
产品介绍
Droxinostat (NS 41080) 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂。Droxinostat 选择性抑制 HDAC3、HDAC6 和 HDAC8,其IC50值分别为 16.9 μM、2.47 μM 和 1.46 μM。Droxinostat 可用于肝细胞癌 (HCC) 的研究。
生物活性

Droxinostat (NS 41080) is ahistone deacetylase (HDAC)inhibitor. Droxinostat selectively inhibitsHDAC3,HDAC6, andHDAC8withIC50values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively. Droxinostat can be used for the research of hepatocellular carcinoma (HCC)[1][2].

IC50& Target[2]

HDAC8

1.46 μM (IC50)

HDAC6

2.47 μM (IC50)

HDAC3

16.9 μM (IC50)

体外研究
(In Vitro)

Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC50values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively[1].
Droxinostat (0, 10, 20, or 40 μM; 48 h) suppresses HDAC3 expression and induces acetylation of histones H3 and H4[2].
Droxinostat (0, 10, 20, 40, and 80 μM; 0, 24, 48, 72, 96, and 120 h) inhibits cell proliferation and colony formation in HepG2 and SMMC-7721 cells[2].
Droxinostat (0 to 80 μM; 48 h) induces hepatoma cell apoptosis by activating mitochondrial apoptotic pathways and downregulating FLIP[2].

Western Blot Analysis[2]

Cell Line:SMMC-7721 and HepG2 (Human liver carcinoma cell lines)
Concentration:0, 10, 20, or 40 μM
Incubation Time:48 h
Result:Significantly decreased the expression of HDAC3 with dose-dependent in HepG2 and SMMC-7721 cell lines.
Significantly enhanced the expression of acetyl-H3 (Ac-H3) and acetylH4 (Ac-H4) in HepG2 and SMMC-7721 cells in a dose-dependent manner.
Upregulated the levels of phospho-p53 and cleaved caspase 3 protein and downregulated the levels of Bcl-2.
Markedly increased the Bax/Bcl-2 ratio in a dose-dependent manner and increased the expression of cleaved PARP protein in HepG2 cells in a dose-dependent manner.
Significant reduced the FLIP expression and enhanced caspase 8 activity in both HepG2 and SMMC-7721cell.

Cell Proliferation Assay[2]

Cell Line:SMMC-7721 and HepG2
Concentration:0, 10, 20, 40, and 80 μM
Incubation Time:0, 24, 48, 72, 96, and 120 h
Result:Decreased the viability with a time-and dose-dependent in both cell lines.

Apoptosis Analysis[2]

Cell Line:SMMC-7721 and HepG2
Concentration:0 to 80 μM
Incubation Time:48 h
Result:Clearly led to dose-dependent apoptosis, but did not induce hepatoma cell apoptosis at 10 μM and had an apoptotic effect at a starting concentration of 20 μM.

RT-PCR[2]

Cell Line:SMMC-7721 and HepG2
Concentration:20 μM and 40 μM
Incubation Time:48 h
Result:Significantly increased the mRNA levels of Bax and p53 genes associated with the mitochondrial p53 apoptosis pathway in a dose-dependent manner in HepG2 and SMMC-7721 cells.
Significantly increased the Bcl-2 mRNA levels in SMMC-7721 cells at a concentration of 40 uM and also increased the Bax/Bcl-2 mRNA ratio.
分子量

243.69

性状

Solid

Formula

C11H14ClNO3

CAS 号

99873-43-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 150 mg/mL(615.54 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.1036 mL20.5179 mL41.0357 mL
5 mM0.8207 mL4.1036 mL8.2071 mL
10 mM0.4104 mL2.0518 mL4.1036 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (10.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.26 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (10.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.26 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (10.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.26 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。