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Sodium 4-Phenylbutyrate

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Chemical Structure| 1716-12-7 同义名 : 4-苯基丁酸钠盐 ;4-PBA sodium;4-Phenylbutyric acid sodium;TriButyrate;NSC 657802;Benzenebutanoic Acid;NaPB;4-Phenylbutyric acid;Sodium Phenylbutyrate;4-PBA;Benzenebutyric acid sodium
CAS号 : 1716-12-7
货号 : A455726
分子式 : C10H11NaO2
纯度 : 98%
分子量 : 186.18
MDL号 : MFCD00800247
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 100 mg/mL(537.11 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • HDAC
描述 Sodium 4-Phenylbutanoate (Sodium Phenylbutyrate) is the sodium salt of phenylbutyrate, a derivative of the short-chain fatty acid butyrate, with potential antineoplastic activity. Phenylbutyrate reversibly inhibits class I and II histone deacetylases (HDACs), which may result in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations. Sodium 4-phenylbutanoate (NaPB) can induce cellular differentiation and cell cycle arrest. NaPB treatment led to time dependent growth inhibition in hepatocellular carcinoma cells Bel-7402. NaPB treatment caused a significant decline in the fraction of S phase cells and a significant increase in G0/G1 cells. NaPB increased the expression of P21(WAF1/CIP1) and E-cadherin in Bel-7402 and significantly decreased the level of HDAC4 in Bel-7402. NaPB significantly improved the level of acetylating histone H4[3]. Pre- or post-treatment with 4-PBA at therapeutic doses attenuated infarction volume, hemispheric swelling, and apoptosis and improved neurological status in a mouse model of hypoxia-ischemia. Moreover, 4-PBA suppressed ER-mediated apoptosis by inhibiting eukaryotic initiation factor 2alpha phosphorylation, CCAAT/enhancer-binding protein homologous protein induction, and caspase-12 activation. 4-PBA could protect against cerebral ischemia through inhibition of ER stress-mediated apoptosis and inflammation[4]. 4-phenylbutyrate protects cells from the deleterious effects of ER(endoplasmic reticulum)-retained aggregated mutant myocilin[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A498 cells 4 mM Function assay 8-48 h Induction of CAMP mRNA expression in human A498 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis 19770273
Hela cells Function assay Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay 19520580
HT-29 cells 4 mM Function assay 8-48 h Induction of CAMP mRNA expression in human HT-29 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis 19770273
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00999167 Cirrhosis Hep... 展开 >>atic Encephalopathy 收起 << Phase 2 Completed - -
NCT01135680 Drug Toxicity Phase 1 Completed - United States, Wisconsin ... 展开 >> Covance Clinical Pharmacology, Inc. Madison, Wisconsin, United States, 53704 收起 <<
NCT00999167 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.37mL

1.07mL

0.54mL

26.86mL

5.37mL

2.69mL

53.71mL

10.74mL

5.37mL
参考文献

[1]Gardian G, Yang L, Cleren C, Calingasan NY, Klivenyi P, Beal MF. Neuroprotective effects of phenylbutyrate against MPTP neurotoxicity. Neuromolecular Med. 2004;5(3):235-41.

[2]Goh M, Chen F, Paulsen MT, Yeager AM, Dyer ES, Ljungman M. Phenylbutyrate attenuates the expression of Bcl-X(L), DNA-PK, caveolin-1, and VEGF in prostate cancer cells. Neoplasia. 2001 Jul-Aug;3(4):331-8.

[3]Wang CT, Meng M, Zhang JC, Jin CJ, Jiang JJ, Ren HS, Jiang JM, Qin CY, Yu DQ. Growth inhibition and gene induction in human hepatocellular carcinoma cell exposed to sodium 4-phenylbutanoate. Chin Med J (Engl). 2008 Sep 5;121(17):1707-11

[4]Qi X, Hosoi T, Okuma Y, Kaneko M, Nomura Y. Sodium 4-phenylbutyrate protects against cerebral ischemic injury. Mol Pharmacol. 2004 Oct;66(4):899-908

[5]Yam GH, Gaplovska-Kysela K, Zuber C, Roth J. Sodium 4-phenylbutyrate acts as a chemical chaperone on misfolded myocilin to rescue cells from endoplasmic reticulum stress and apoptosis. Invest Ophthalmol Vis Sci. 2007 Apr;48(4):1683-90