Droxinostat

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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。

CAS NO:

99873-43-5

NS 41080

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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	4.1036 mL	20.5179 mL	41.0357 mL
5 mM	0.8207 mL	4.1036 mL	8.2071 mL
10 mM	0.4104 mL	2.0518 mL	4.1036 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。