漆树酸作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAnacardic AcidCat. No.: HY-N2020CAS No.: 16611-84-0分式: CHO分量: 348.52作靶点: Histone Acetyltransferase; Epigenetic Reader Domain; Bacterial作通路: Epigenetics; Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (286.93 mM; Need u

2、ltrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.8693 mL 14.3464 mL 28.6928 mL5 mM 0.5739 mL 2.8693 mL 5.7386 mL10 mM 0.2869 mL 1.4346 mL 2.8693 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-

3、20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 10 mg/mL (28.69 mM); Clear solution此案可获

4、得 10 mg/mL (28.69 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (28.69 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemE此案可获得 10 mg

5、/mL (28.69 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。以 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 10 mg/mL (28.69 mM); Clear solution此案可获得 10 mg/mL (28.69 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄 DMSO 储备液加到 900 L

6、 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Anacardic Acid是从从腰果壳中提取液中分离到的酸类物质，为 histone acetyltransferases 抑制剂，对 p300 和 PCAF的 IC50 值分别为 -8.5 M 和 -5 M。IC & Target p3008.5 M (IC50)体外研究 Anacardic Acid is a histone acetyltransferase, inhibits HAT activity of p300 and PCAF, with IC50s of -8.5 M and -5 M,respectively

7、1. Anacardic Acid (300 M) inhibits mycelial growth. Anacardic Acid (50 M) induces apoptosis-likecharacteristics in M. oryzae, and the effect is caspase independent. Anacardic Acid (1-80 M) leads to loss ofmitochondrial potential. Anacardic Acid (1-60 M) also exhibits antioxidant activity in M. oryza

8、e3.体内研究 Anacardic acid (5 mg/kg, i.p.) attenuates the binding of HATs to the promoter of MEF2A and reverse hyperacetylationof H3K9ac caused by phenylephrine in C57BL/6 mice. Anacardic acid inhibits the level of transcription on MEF2A and cardiac development-related downstream genes, attenuates the p

9、rotein overexpression of cardiac downstream genescaused by phenylephrine, reverses and attenuates cardiac hypertrophy in the hearts of mice exposed tophenylephrine, and attenuates the left ventricular pressure and improves cardiac function in the cardiac hypertrophymice2.PROTOCOLKinase Assay 1 Brief

10、ly, indicated amounts of proteins/peptide are incubated in HAT assay buffer containing 50 mM Tris-HCl, pH 8.0,10% (v/v) glycerol, 1 mM dithiothreitol, 1 mM phenylmethyl sulfonyl fluoride, 0.1 mM EDTA, pH 8.0, 10 mM sodiumbutyrate at 30C for 10 min in the presence or absence of compound followed by t

11、he addition of 1 L of 6.2 Ci/mmol3Hacetyl coenzyme A (acetyl-CoA) and are further incubated for another 10 min. The final reaction volume is 30 L.The reaction mixture is then blotted onto P-81 filter papers, and radioactive counts are recorded on a Wallac 1409liquid scintillation counter. To charact

12、erize the inhibition kinetics of anacardic acid, filter binding assays are doneusing a constant amount of HeLa core histones in the presence or absence of AA with increasing concentrations of 3Hacetyl-CoA1.MCE has not independently confirmed the accuracy of these methods. They are for reference only

13、.Cell Assay 3 Mycelial cell death assay is performed to evaluate the number of colony-forming units in treated and untreated samples. M. oryzae conidia (106 conidia/mL) are allowed to germinate in 100-mL flasks with 20 mL completemedium broth (CM) at 28C in a rotary shaker (200 rpm) for 12 h. The cu

14、ltures are exposed to differentconcentrations of anacardic acid for 2 h. The germinated conidia are washed with sterile water, diluted to 104conidia/mL, and plated on oat meal agar and incubated at 28C for 3 days. Colony-forming units (CFUs) are countedin each of the three ndividual experiments perf

15、ormed, and values are plotted in the graph as average of threereplicates. The data in each sample is expressed as the percentage of the total number of CFUs observed in untreatedPage 2 of 3 www.MedChemEor 0.1 % DMSO treated control3.MCE has not independently confirmed the accuracy of these methods.

16、They are for reference only.Animal Pathogen-free male and female 11-13 week-old C57BL/6 mice (18-20 g) are randomly selected to injectAdministration 2 phenylephrine (20 mg/kg) (control groups receive equivalent normal saline). In some cases, phenylephrine-treatedC57BL/6 mice are administered with a

17、Chinese herbal extract anacardic acid (5 mg/kg). Anacardic acid is dissolved insterile DMSO at a concentration of 1 mg/ml and stored at 4C. Phenylephrine is administered by a subcutaneousinjection at a dose of 20 mg per kg per day continuously for 30 days. Moreover, anacardic acid is administered by

18、 anintraperitoneal injection at a dose of 5 mg/kg every 3rd day intraperitoneal injection at a dose of 5 mg/kg every 3rdday. After modeling, mice are euthanized using 20% carbon dioxide in an anesthesia chamber until they areunresponsive to nose pinch and the hearts are isolated2.MCE has not indepen

19、dently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 FASEB J. 2019 May 3:fj201802575RR. Patent. US20180263995A1.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Balasubramanyam K, et al. Small molecule modulators of histone acetyltransferas