|N-羟基-4-(2-((2-羟乙基)(ph苯基)氨基)-2-氧乙基)苯甲酰胺|CsnPharm

CAS No.: 1429651-50-2

N-Hydroxy-4-(2-((2-hydroxyethyl)(phenyl)amino)-2-oxoethyl)benzamide Catalog No. CSN18800

Synonyms: HPOB

HPOB is a selective inhibitor of HDAC6 with IC50 of 56 nM.

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实验方案

技术信息

生物活性

描述HPOB is a selective HDAC6 inhibitor with IC50 value of 56nM, exhibiting at least 30-fold selectivity to HDAC6 over other HDACs. Treatment with HPOB at concentration of 8-32μM for 72h led to cell growth inhibition of normal (HFS) and transformed (LNCaP, A549, and U87) cells but did not induce cell death. HPOB at concentration of 4-16μM caused accumulation of acetylated α-tubulin and acetylated peroxiredoxin, both of which are HDAC6 substrates, in normal (HFS) and transformed (LNCAP, U87, and A549) cells post 24-hour treatment, without effect on acetylated histones. HPOB only inhibited the catalytic activity but not the ubiquitin-binding activity of HDAC6. HPOB had the therapeutic potential in combination therapy to enhance the potency of anticancer drugs including, etoposide, doxorubicin and SAHA in vitro, and enhance anticancer effects of SAHA (50mg/kg) in mice bearing human prostate cancer CWR22 xenograft at dose of 300mg/kg, i.p., for 25 days.
动物研究
剂量
Mice: 100 mg/kg - 300 mg/kg^[2] (i.p.)

给药途径
i.p.
临床研究

动物研究
剂量	Mice: 100 mg/kg - 300 mg/kg^[2] (i.p.)
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01455363	Carcinoma, Basal Cell	Not Applicable	Completed	-	France ... more >> Institut Curie Paris, France, 75005 Collapse <<

参考文献

[1] Li ZY, Li QZ, et al. HPOB, an HDAC6 inhibitor, attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway. Neurochem Int. 2016 Oct;99:239-251.
[2] Lee JH, Mahendran A, et al. Development of a histone deacetylase 6 inhibitor and its biological effects. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9.

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
- 3.1813 mL
- 15.9066 mL
- 31.8131 mL
- 5 mM
- 0.6363 mL
- 3.1813 mL
- 6.3626 mL
- 10 mM
- 0.3181 mL
- 1.5907 mL
- 3.1813 mL

技术信息

CAS号

1429651-50-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H18N2O4

运输

蓝冰

分子量

314.34

别名

HPOB

溶解度

DMSO	62.0 mg/mL (197.2 mM)
Water	Insoluble
Ethanol	38.0 mg/mL (120.9 mM) warming

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N-Hydroxy-4-(2-((2-hydroxyethyl)(phenyl)amino)-2-oxoethyl)benzamide Catalog No. CSN18800

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