Valproic-acid-VPA-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEValproic acidCat. No.: HY-10585CAS No.: 99-66-1Synonyms: VPA; 2-Propylpentanoic Acid分式: CHO分量: 144.21作靶點(diǎn): HDAC; Autophagy; Mitophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy儲(chǔ)存式: Pure form -20C 3 years4C 2 yearsIn solven

2、t -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (693.43 mM; Need ultrasonic)H2O : 1 mg/mL (6.93 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 6.9343 mL 34.6717 mL 69.3433 mL5 mM 1.3869 mL 6.9343 mL 13.8687 mL10 mM 0.6934 mL 3.4672 mL 6.9343 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解

3、度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3.25 mg/mL (22.54 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD

4、 in saline)Solubility: 3.25 mg/mL (22.54 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3.25 mg/mL (22.54 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Valproic acid種 HDAC 抑制劑，IC50 值為 0.5-2 mM，抑制 HDAC1 的活性，(IC50，400 M)，同時(shí)可誘導(dǎo) HDAC2 的降解；V

5、alproic acid sodium salt 可于癲癇、雙相情感障礙和偏頭痛等的研究。IC50 & Target HDAC1 HDAC HDAC2 Autophagy400 M (IC50) 0.5-2 mM (IC50)Mitophagy體外研究 Valproic acid inhibits the growth dose- and time-dependently with an IC50 of appr 10 and 4 mM at 24 and 72h, respectively. Valproic acid significantly attenuates the activit

6、ies of total, cytosol and nuclear HDACs.Valproic acid increases the form of acetylated histone 3 in HeLa cells. Valproic acid (1-3 mM) induces a G1phase arrest, while 10 mM Valproic acid significantly induces a G2/M phase arrest of cell cycle in HeLa cells.In addition, Valproic acid increases the pe

7、rcentage of sub-G1 cells in HeLa cells in a dose-dependentmanner at 24 h 1. Valproic acid inhibits the mRNA and protein expression of VEGF, VEGFR2 and bFGF.Valproic acid inhibits the protein expression of HDAC1, increases histone H3 acetylation, and enhances theaccumulation of hyperacetylated histon

8、e H3 on VEGF promoters 2. Valproic acid treatment results inincreased levels of phosphorylated AMPK/ACC in primary mouse hepatocytes. Phosphorylation of ACCfollowing Valproic acid treatment is AMPK-dependent. Valproic acid inhibits the deacetylase activity of bothmouse liver nuclear extracts and hum

9、an recombinant HDAC1 while of the metabolites of Valproic acid, only2-ene-Valproic acid and 4-ene-Valproic acid diminish deacetylase activity 4.體內(nèi)研究 Valproic acid (500 mg/kg, i.p.) inhibits the tumor growth and angiogenesisin the mice transplanted withKasumi-1 cells. The IR rate in the Valproic acid

10、 group is 57.25% at the end of the experiment 2. Valproicacid (350 mg/kg, i.p.) demonstrates more social investigation and play fighting than control animals 3.PROTOCOLKinase Assay 1 The activity of caspase-3, -8 and -9 is assessed using the caspase-3, -8 and -9 colorimetric assay kits,respectively.

11、 In brief, 1106 cells in a 60-mm culture dish are incubated with 10 mM Valproic acid for 24 h.The cells are then washed in PBS and suspended in 5 volumes of lysis buffer provided with the kit. Proteinconcentrations are determined using the Bradford method. Supernatants containing 50 g total protein

12、areused to determine caspase-3, -8 and -9 activities. The supernatants are added to each well in 96-wellmicrotiter plates with DEVD-pNA, IETD-pNA or LEHD-pNA as caspase-3, -8 and -9 substrates and the platesare incubated at 37C for 1 h. The optical density of each well is measured at 405 nm using a

13、microplatereader. The activity of caspase-3, -8 and -9 is expressed in arbitrary absorbance units.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemECell Assay 1 In brief, 5105 cells are seeded in 96-well mi

14、crotiter plates for MTT assays. After exposure to the designateddoses of Valproic acid for the indicated times, MTT solution 20 mL: 2 mg/mL in phosphate-buffered saline(PBS) is added to each well of the 96-well plates. The plates are additionally incubated for 3 h at 37C.Medium is withdrawn from the

15、 plates by pipetting and 200 mL DMSO is added to each well to solubilize theformazan crystals. The optical density is measured at 570 nm using a microplate reader.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Splenectomies are performed on the

16、BALB/c nude mice. One week after the splenectomies, the mice receivAdministration 2 whole body irradiation with 137Cs at a dose of 4 Gy. At 48-72 h post-irradiation, the mice are subcutaneouslyimplanted with Kasumi-1 cells (2107 cells/mouse with 0.15-0.2 mL) in the right axillary region. The mice ar

17、erandomLy assigned to two groups, the Valproic acid (n=6) and control (n=6) groups. When the tumors areappr 200 mm3 in size at appr 10 days post-implantation, 0.2 mL Valproic acid (500 mg/kg body weight) or 0.2mL saline is injected intraperitoneally every day. Valproic acid is dissolved in saline at

18、 a concentration of 25mg/mL. The longest diameter (a) and the shortest diameter (b) of the tumor are measured every three days,and the tumor volume (TV) is calculated according to the following formula: TV=1/2ab2. Following twoweeks of injections, the mice are sacrificed by cervical dislocation and

19、the tumor masses are removed for thefollowing experiments.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Biomaterials. 2018 Dec 6;193:30-46.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Han BR, et al. Valproic acid i

20、nhibits the growth of HeLa cervical cancer cells via caspase-dependent apoptosis. Oncol Rep. 2013Dec;30(6):2999-3005.2. Zhang ZH, et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov28.3. Cohen OS, et al. Acute prenatal exposure to a moderate dose of valproic acid increases social behavior an