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1-Naphthohydroxamic acid
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。
1-Naphthohydroxamic acid图片
CAS NO:6953-61-3
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

产品介绍
1-Naphthohydroxamic acid (Compound 2) 是一种有效的,选择性的HDAC8抑制剂,IC50为 14 μM。1-Naphthohydroxamic acid 对HDAC8的选择性高于 I 类 HDAC1 和 II 类 HDAC6 (IC50>100 μM)。1-Naphthohydroxamic acid 不会增加整体组蛋白 H4 的乙酰化,也不会降低总细胞内 HDAC 的活性。1-Naphthohydroxamic acid 可诱导微管蛋白乙酰化。
生物活性

1-Naphthohydroxamic acid (Compound 2) is a potent and selectiveHDAC8inhibitor with anIC50of 14 μM. 1-Naphthohydroxamic acid is more selectively forHDAC8than class IHDAC1and class IIHDAC6(IC50>100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellularHDACactivity[1][2].1-Naphthohydroxamic acid can induce tubulin acetylation[3].

IC50& Target[1]

HDAC8

14 μM (IC50)

HDAC1

>100 μM (IC50)

HDAC6

>100 μM (IC50)

体外研究
(In Vitro)

1-Naphthohydroxamic acid (compound 2; 20-40 μM; 0-144 hours; BE(2)-C, SK-N-BE(2) and SH-SY5Y cells) treatment reduces cell numbers in a concentration-dependent manner[2].
1-Naphthohydroxamic acid (compound 2) at concentrations in the range of its in vitro IC50against HDAC8 results in reduced cell density and outgrowth of neurite-like structures that stained positive for neurofilament.1-Naphthohydroxamic acid reduces the formation of clones in soft-agar concentration dependently[2].
When either cell type (HeLa and HEK293 cells) is treated with 1-Naphthohydroxamic acid (compound 2; 0.8 μM, 4 μM, 20 μM or 100 μM), only tubulin becomes hyperacetylated[1].

Cell Proliferation Assay[2]

Cell Line:BE(2)-C, SK-N-BE(2) and SH-SY5Y cells
Concentration:20 μM, 40 μM
Incubation Time:0 hours, 24 hours, 48 hours, 72 hours, 96 hours, and 144 hours
Result:Reduced cell numbers in a concentration-dependent manner.
体内研究
(In Vivo)

Dose-limiting toxicities (DLTs) of 1-Naphthohydroxamic acid (compound 2; 0-40 mg/kg; intraperitoneal injection; daily; for 10 day; NMRIFoxn1nude mice) include weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination. 1-Naphthohydroxamic acid has the maximum tolerable doses at 50 mg/kg per day. At these concentrations, neither body weight nor blood parameters are critically changed[3].
Pharmacokinetic studies after intraperitoneal administration of the inhibitors identified the half-life of 1-Naphthohydroxamic acid to be ~15 min, with a plasma peak concentration of ~30 μM[3].

Animal Model:NMRIFoxn1nude mice[3]
Dosage:0 mg/kg, 50 mg/kg, 100mg/kg, 200 mg/kg, 300 mg/kg 400 mg/kg
Administration:Intraperitoneal injection; daily; for 10 days
Result:Dose-limiting toxicities (DLTs) included weight loss and signs of liver toxicity, as evidenced by elevated plasma liver enzymes and detection of necrotic areas on histological liver examination.
分子量

187.19

性状

Solid

Formula

C11H9NO2

CAS 号

6953-61-3

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 : 125 mg/mL(667.77 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM5.3422 mL26.7108 mL53.4217 mL
5 mM1.0684 mL5.3422 mL10.6843 mL
10 mM0.5342 mL2.6711 mL5.3422 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。