Meleagrin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MIC: 32-64 μg/ml for S. aureus, E. coli, and S. pneumoniae
Meleagrin is an antibiotic.
Meleagrin is an antibiotic derived from a deep ocean, penicillin-producing P. chrysogenum.
In vitro: It was found that consistent with their selective inhibition of Staphylococcus aureus FabI, meleagrin and its more active derivatives could directly bind to S. aureus FabI that was measured in a fluorescence quenching assay, inhibit intracellular fatty acid biosynthesis and growth of S. aureus, and increase the minimum inhibitory concentration (MIC) for fabI-overexpressing S. aureus. The compounds that were not effective against the FabK isoform, however, were able to inhibit the growth of Streptococcus pneumoniae containing only the FabK isoform. In addition, no resistant mutant to these compounds was obtained. Notely, fabK-overexpressing Escherichia coli was found to be not resistant to these compounds, but was resistant to triclosan [1]. Another study found that meleagrin was able to inhibit the growth of the human breast cancer cell lines, while similar treatment doses had no effect on the growth and viability of the non-tumorigenic human mammary epithelial cells MCF10A. Meleagrin also displayed good ATP competitive c-Met inhibitory activity in Z-Lyte assay [2].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Zheng, C. J.,Sohn, M.J.,Lee, S., et al. Meleagrin, a new FabI inhibitor from Penicillium chryosogenum with at least one additional mode of action. PLoS One 8(11), (2013).
[2] Mady MS et al. The indole alkaloid meleagrin, from the olive tree endophytic fungus Penicillium chrysogenum, as a novel lead for the control of c-Met-dependent breast cancer proliferation, migration and invasion. Bioorg Med Chem. 2016 Jan 15;24(2):113-22.
Physical Appearance | A light tan to tan solid |
Storage | Store at -20°C |
M.Wt | 433.5 |
Cas No. | 71751-77-4 |
Formula | C23H23N5O4 |
Synonyms | 6-O-Methyloxaline |
Solubility | Soluble in ethanol;Soluble in methanol;Soluble in DMSO;Soluble in dimethyl formamide |
Chemical Name | (3E,7aR,12aS)-7a-(1,1-dimethyl-2-propen-1-yl)-7a,12-dihydro-6-hydroxy-3-(1H-imidazol-5-ylmethylene)-12-methoxy-1H,5H-imidazo[1',2':1,2]pyrido[2,3-b]indole-2,5(3H)-dione |
SDF | Download SDF |
Canonical SMILES | OC1=CC2(C(C)(C)C=C)C3(N(OC)C4=C2C=CC=C4)N(/C(C(N3)=O)=C\C5=CNC=N5)C1=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
人类乳腺癌细胞系 |
溶解方法 |
在DMSO中是可溶的。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
0~50 μM |
应用 |
Meleagrin抑制人乳腺癌细胞MDA-MB-231,MDA-468,BT-474,SK BR-3,MCF7和MCF7-dox的生长,同时发现相似的治疗剂量对非致瘤性人乳腺上皮细胞MCF10A的生长和生存力没有影响。Meleagrin在Z-Lyte分析中还表现出出色的ATP竞争性c-Met抑制活性,这已通过分子对接研究和Western blot分析进一步证实。 |
References: [1]. Mady MS, Mohyeldin MM, Ebrahim HY, Elsayed HE, Houssen WE, Haggag EG, Soliman RF, El Sayed KA. The indole alkaloid meleagrin, from the olive tree endophytic fungus Penicillium chrysogenum, as a novel lead for the control of c-Met-dependent breast cancer proliferation, migration and invasion. Bioorg Med Chem. 2016 Jan 15;24(2):113-22. doi: 10.1016/j.bmc.2015.11.038. Epub 2015 Nov 28. PMID: 26692349; PMCID: PMC4703546. |