表观遗传化合物库 (Epigenetics Compound Library)
Epigenetics Compound Library目录
Identification of bioactive HDAC inhibitors in bovine cardiac tissue. Bovine cardiac tissue was treated with increasing concentrations of indicated nonflavonoids (A and B) and flavonoids (C and D) for 2 h. Bovine cardiac tissue was subsequently incubated with fluorogenic HDAC substrates for 2 h prior to addition of stop solution for 20 min. Fluorescence was assessed via BioTek Synergy plate reader and demonstrated pan-HDAC inhibition of all compounds.
Mol Nutr Food Res, 2016.. purchased from Selleck
Scatter plot from phenotypic kinase inhibitor screen T. brucei 221 strain showing duplicate screens for the 274 compounds used in the phenotypic screened at 1 μM. Black dots represent results from first independent screen (221A) and grey dots represent results from second screen (221B). Dotted line represent cut-off point for 3 standard deviation below the mean (solid black line).
Bioorg Med Chem, 2016, 24(19):4647-51.. purchased from Selleck
Epigenetic chemical compound library screen for the effect of 24 compounds on adipocytic differentiation of human skeletal (mesenchymal) stem cells (hMSCs). Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 after treatment with the indicated compounds (500 nM). Images were taken at 320 magnification using a Zeiss inverted microscope. Abbreviation: DMSO, dimethyl sulfoxide.
Stem Cells Transl Med, 2016, 5(8):1036-47.. purchased from Selleck
Compound screening and confirmation. (A) High-throughput screening of CHIKV 26S mediated insect cell fusion inhibitors obtained from a library of 788 FDA-approved drugs. (B) Microneutralization assay. The square frame represents the protective effects of niclosamide and nitazoxanide against CHIKV-induced CPE. (VC: as CHIKV infection control, CC: as negative control.)
Antiviral Res, 2016, 135:81-90.. purchased from Selleck
(c) Dot plot summarizes the results of Phase I EpI screen. y-Axis indicates cell viability and x-axis represents induction of Ecad promoter activity. Five drugs, Vorinostat, Bortezomib, Etravirine, Niclosamide and Crystal violet, were identified with more than twofold Ecad promoter activity. (d) Dot plot summarizes the results of Phase 2 screen on HDAC inhibitors.
Cell Death Discov, 2016, 2:16041.. purchased from Selleck
Hit compounds display varying effects on p‐EGFR and EGFR levels. Of 21 EGFR/ERBB hit compounds that selectively targeted chordoma cells, the impact of 13, comprising a selection of hit compounds across the libraries and chemical structures tested, was studied by western blot on three chordoma cell lines (U-CH1, U-CH2, MUG-Chor1). Cells were serum‐starved overnight before being treated with EGFR inhibitors (250 nm) for 4 h and then being exposed to EGF (50 ng/ml) for 15 min.
J Pathol, 2016, 239(3):320-34.. purchased from Selleck
Results of clinical collection compound primary screen. Panel A. Scatterplot representing the results for the screen at 5 μM. Green circles represent the hits, blue circles are all the other compounds. Panel B. Scatterplot representing the results for the screen at 15 μM. Green circles represent the hits from the 5 μM screen, blue circles are all the other compounds. Panel C. Scatterplot comparing T. cruzi percent inhibition between 5 μM and 15 μM screens. Panel D. Replicates plot for a subset of compounds screened twice at 5 μM (n = 579, R2 = 0.86).
PLoS Negl Trop Dis, 2016, 10(4):e0004584.. purchased from Selleck
Graphical representation of hit compounds that block cardiomyocyte hypertrophy. (A) Compounds from the Spectrum Library are depicted based on percent inhibition of ANF expression (X-axis) and cell area (Y-axis) relative to the positive control HDAC inhibitor, TSA; % inhibition by TSA was set to 100% for each plate. Reduction in the number of identified cells (nuclei) compared to the positive control TSA was used as an indicator of toxicity. Toxic compounds are indicated in red, and were removed from subsequent analysis. (B) Class I hits are those compounds that significantly reduce cell area and ANF expression. Class II hits are compounds that significantly reduce cell area, but increase ANF expression.
J Mol Cell Cardiol, 2016, 97:106-13.. purchased from Selleck
Screening small molecule library in 384-well plates. (A): Schematic diagram of HTS screening of small molecule library. (B): Screening results of an epigenetics library. Each heat map represents one 384-well plate treated with the epigenetics library in duplicate wells at specified concentration(0.1, 1 and 10 μM). Wells G11 and K11 were duplicate wells of 5-aza-C. Wells K7 and L7 were duplicate wells of 5-aza-dC.
Stem Cells, 2017, 35(1):158-169.. purchased from Selleck
(c) Percentage of H3.3S31ph positive cells after treatment with candidate compound hits identified from the inhibitor library screen. The targets of inhibitors are the following: WZ3146: EGFR; Sorafenib Tosylate: VEGFR, PDGFR, and RAF/MEK/ERK; AT7519: CDK1, 2, 4, 5, 6, and 9; Hesperadin, AZD1152-HQPA, and ZM447439: AURKB; AZD8055 and KU-0063794: mTOR; MK-2206: Akt1, 2, and 3; GSK2126458: PI3K and mTOR.
J Mol Biol, 2017. . purchased from Selleck