Anti-diabetic Compound Library
A unique collection of 29 anti-diabetes compounds under clinical trials
Anti-diabetic 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
Plots of locomotor seizure behaviour for 5 dpf scn1Lab mutants screened against (A) 52 ion channel ligands. Threshold for inhibition of seizure activity (positive hits) was determined as a reduction in mean swim velocity of 540% (red line). Blue data points represent compounds that were classified as toxic as treated larvae have no visible heartbeat or movement in response to touch after 90-min exposure.
Brain, 2017.. purchased from Selleck
Plots of locomotor seizure behaviour for 5 dpf scn1Lab mutants screened against (B) 254 compound GPCR ligands. Threshold for inhibition of seizure activity (positive hits) was determined as a reduction in mean swim velocity of 540% (red line). Blue data points represent compounds that were classified as toxic as treated larvae have no visible heartbeat or movement in response to touch after 90-min exposure.
Brain, 2017.. purchased from Selleck
The screening of Aβ40 inhibitors using AD models.(a) Scheme showing the cell culture procedure of chemical screening. (b) The result of first screening of Aβ40 inhibitors. The red line shows the value of the average ratio minus double the standard deviation (Ave - 2SD = 0.33). The compounds that reduced the Aβ40 ratio below Ave - 2SD value (0.33) passed the first screening. The Aβ40 level of DMSO treatment was considered to be 1.0. (c) The result of second screening in Aβ40 inhibitors. The red line indicates the criterion of hit compounds in the second screening (=0.5). (d,e) The effects of Aβ inhibition (d) and cell survival (e) in dose-response experiments using K1-derived neurons. These results show that PS1-overexpression did not influence the screening of Aβ inhibitors. The numerical data is shown in Supplementary Table S2. The amount of Aβ40 and cell viability in DMSO-treated PS1-G378E or K1 neurons was defined as 1.0. *P < 0.05, as determined by Steel’s test. Three independent experiments, each time in triplicates were performed (n = 3). Values are Mean ± SD. AraC, cytosine arabinoside; G378E, PS1-G378E neurons; K1, KhES-1-derived neurons; Nilo, Nilotinib; Pime, Pimecrolimus; Rosu, Rosuvastatin Calcium; Sulc, Sulconazole Nitrate salt; Tore, Toremifene Base.
Sci Rep, 2016, 6:33427.. purchased from Selleck
(A)Schematic view of virtual screening workflow on human ABCB1 and human ABCG2. (B) The sensitization effects of virtual screened compounds on SW620/Ad300 towards doxorubicin. (C) The sensitization effects of virtual screened compounds on NCI-H460/MX20 cells towards mitoxantrone. (D) Chemical structure of bafetinib.
Sci Rep, 2016, 6:25694.. purchased from Selleck
The results of the high-throughput screening (HTS) of 1017 FDA-approved drugs in the DSP assay for MERS-S. Screening results of 1017 drugs using the HTS DSP assay. (A) The vertical axis shows the reading of the DSP activity (RL activity) for the tested drugs (1 μM). The RL values were normalized to the control, which contained DMSO only. The horizontal axis represents the identification number arbitrarily assigned to each drug. Each dot represents an individual drug. The dotted line indicates 20% of the control. The value of the most active drug, nafamostat, is indicated (1.66% of the control).
Antimicrob Agents Chemother, 2016, 60(11):6532-6539.. purchased from Selleck
Relative wound density and cell viability z-score data of the shortlisted candidates from the primary screening assay. Based on their effect on migration and cell viability, the drugs were binned into high confidence and medium confidence migration and cytotoxic classes. a The migration z-score of the candidates are shown, drugs with a z-score between the dotted line (-1.6) and the straight line (–2) were binned into medium confidence migration class and the drugs with z-scores beyond the straight line (<-2) were binned as.
Clin Exp Metastasis, 2016, 33(4):385-99.. purchased from Selleck
Screen of library of FDA-approved library validates the adenylate kinase assay and indicates it is more sensitive than growth-based assays. A. Scatter plot of raw data from primary screen of the Selleck FDA-approved drug library. The cut-off for hit identification (2-fold increase in AK activity) is indicated by the solid line.
PLoS One, 2015, 10(6):e0129234.. purchased from Selleck
355 compounds from the Selleck library were docked into the six generated PRK1 homology models, the obtained docking poses were minimized using an implicit solvent model, and BFE calculation was subsequently performed. The predicted pIC50 was calculated using the developed QSAR model.
ChemMedChem, 2016, 11:1-12.. purchased from Selleck
Chemical screen targeting erythroid enucleation. (B) For the compound screen orthochromatic erythroblasts were isolated by FACS and subsequently incubated in 96-well plates in the presence of the compounds for 5h. The extent of enucleation was assessed by FACS LSR II. Graphs showing that the raw data between the duplicate assay plates are reproducible. (C) Graph showing compounds confirmed to significantly (paired student's t-test) inhibit enucleation compared to the vehicle control (DMSO). Data are means (+/− SD) of 4 independent experiments. *P< 0.05, **P< 0.01, ***P< 0.001, ****P< 0.0001 (paired student's t-test).
purchased from Selleck
Anti-ferroptosis activity of natural product. PANC1 cells were treated with erastin (20 mM) in the absence or presence of the indicated natural product compounds (10 mM). Cell viability was assayed using the CCK-8 kit
Biochem Biophys Res Commun, 2016, 473(4):775-80.. purchased from Selleck
Discovery of small-molecule inhibitors of MST3 using DSF. a) Distribution of compounds as a function of △Tm values. Of the 277 compounds screened, 23 compounds interfered with the assay due to intrinsic fluorescence or precipitation and were discarded from further evaluation; 109 compounds showed negative temperature shifts (-2.8 to -0.01℃) and were denoted as zero. Each bar represents compounds with △Tm ≤x-axis value, that is, 0: △Tm≤0; 1: △Tm≤1, etc. b) Identifiers and associated IC50 and △Tm values of compounds confirmed as MST3 binders by X-ray crystallography. c) Logarithmic proportionality between DTm and IC50 values; data were fit to Equation (1), yielding y0=4.08±0.3 and a=-0.93±0.09.
ChemMedChem, 2016, 11(11):1137-44.. purchased from Selleck
Hits of high throughput in vitro drug screen of three MLS cell lines. List of 27 drugs with a reduction in cell viability of >50% in two or all three cell lines at a drug concentration of 100 nM. Strong inhibitory effect of the survivin inhibitor YM155 is observed in two out of three MLS cell lines. Also, a good response is observed to several conventional chemotherapeutics, like doxorubicin, gemcitabine, and paclitaxel. Per drug, four concentrations (1, 10, 100, and 1000 nM) are tested; green boxes correspond to a high cell viability (~100%) and red boxes to a loss of cell viability (~0%). For comparison, at the bottom, five compounds are randomly shown that did not meet the criteria.
Transl Oncol, 2017, 10(4):546-554. purchased from Selleck
CCRF-CEM and Jurkat cells display a differential response to kinase inhibitors: Cells were treated with 100 nM (A) and 1000 nM (B) concentration of a panel of kinase inhibitors (378 inhibitors) for two days. Cell viability was measured using PrestoBlue cell viability assay. Selective inhibitors from “A” and “B” were used in figure "C" and "D".
Cancer Lett, 2017, 405:73-78. purchased from Selleck
The impact of FDA-approved drugs on ERa levels in MCF-7 cells. (A) Pie diagrams depicting the pharmaceutical categories in the library. (B) Synthetic protocol used for drug administration to MCF-7 cells. (C) Assay data depicting the quantitation of ERa levels in each one of the 162 performed Western blots. Z0 is the Z factor for negative (DMSO) and positive (E2) controls in each Western blot analysis. Robust Z scores (Z*) graphs for drug-treated samples alone (D), in combination with E2 (E) or for the effect of E2 within each drug-treated sample (i.e., E2þdrug/drug alone) (F); red arrows indicate the Z* for drugs considered as positive hits. Red lines indicate the threshold used for analysis. Western blot analyses of ERa and cathepsin D (Cat D) expression levels in MCF-7 cells treated for 24 h with E2 (1 nM) both in the presence or in the absence of 100 nM estriol (ESTR) (G), coumarin (COUM) (G0), basedoxifene (BASE) (H), vinblastine (VINB) (H0) and carfilzomib (CARF) (I) or vehicle (DMSO-CTR). The loading control was done by evaluating vinculin expression in the same filter.
Mol Cell Endocrinol, 2017, S0303-7207(17)30400-8. purchased from Selleck
(A) Schematic representation of the compound screening. J-LAT A2 cells were co-treated with compounds (5 μM) and TNFα (10 ng/ml) for 24 hr. Cells were then stained with Hoechst® 33342 followed by imaging analysis. The assay was performed in quadruplicate. (B) Fluorescence images showing the reactivation (GFP, green) and cell nucleus (blue) in J-LAT A2 cells treated with TNFα for the indicated compounds. Values represent the mean ± s.d. of the % GFP-positive cells (n ≥ 4). (C) Scatter plot of the % GFP-positive cells vs % cell numbers for all tested compounds. Results were normalized to DMSO control. LSM, levosimendan; SPR, spironolactone; 9AA, 9-aminoacridine
Antiviral Res, 2017, 146:76-85. purchased from Selleck
High-throughput luciferase screening to identify parkin inducing compounds. (A) Schematic illustration of the high-throughput screening method. HEK-293T parkin reporter cell line (parkin-LucHEK-293T) was selected by stable transfection of the luciferase construct containing three repeats of parkin promoter’s CREB/ATF4 binding motifs. In a 96-well plate, 1172 FDA-approved drugs were used to treat parkinLuc-HEK-293T cells. Parkin promoter activity was measured by luciferase assay. DMSO was used as a negative control. CCCP treatment was used as a positive control. (B) Parkin promoter activities in parkin-Luc-HEK-293T cell line treated with DMSO or 10uM CCCP as positive control (n=4) were measured by luciferase assay. (C) Scatter plot showing relative increase of parkin promoter activity in parkin-Luc-HEK-293T cell line treated with each compound compared to DMSO negative control based on luciferase assay. Top 20 compounds were highlighted in red color. (D) Relative increase of parkin promoter activity induced by the top 20 compounds based on the initial HTS screening determined by luciferase assay (n=9, see also Table 1). Quantified data are expressed as mean±s.e.m. *P<0.05, **P<0.01, and ***P<0.001, nonparametric Kruskal-Wallis ANOVA test (B) and ANOVA test followed by Tukey post hoc analysis (D).
Sci Rep, 2017, 7(1):525. purchased from Selleck
(c) Results of the second-round test on Aurora kinases inhibitors. Samples are under corresponding treatment for 3 weeks and measured by bioluminescence. CTRL, control. P value is determined by two-tailed unpaired Mann-Whitney U-test with multiple-test correction. N=6 bone fragments in each group. Representative bioluminescence images are shown at the bottom of the panel. (d) Results of the second-round test on HMT inhibitors. Samples are under corresponding treatment for 3 weeks and measured by bioluminescence. P value is determined by two-tailed unpaired Mann–Whitney U-test with multiple-test correction. N=6 bone fragments in each group. Representative bioluminescence images are shown at the bottom of the panel.
Nat Commun, 2017, 8:15045. 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 (128 compounds; see Table S1 for a description of compounds in each well). 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 Heat map of selected anti-cancer compounds exhibiting strong inhibition in at least one of the PDC lines. The scale represents percentage inhibition of the compounds, with inhibition score <50% shown in grey. d Selected molecular signatures (P < 0.05) of genes that show elevated expressions across the five Met cell lines, some of which appear to be associated with the selective responses of PDC lines to compounds of same target classes.
Nat Commun. 2017, 8(1):435. purchased from Selleck
Repurposing Library contents. (a) Highest clinical phase achieved by each compound. 3,422 drugs in the library have reached clinical use as of November 2016. (b) Number of compounds per target category. Compounds with multiple targets might be indicated in more than one category. (c) Number of approved drugs for indications within each listed disease area. (d) Classification of proteins targeted by library drugs. Protein function hierarchy is shown with increasing specificity of function corresponding to distance from the figure center. The relative area of each segment is proportional to the fraction of the Repurposing Library targeting each protein class. As expected, the library is enriched in drugs targeting kinases, GPCRs, and ion channels.
Nat Med, 2017, 23(4):405-408. purchased from Selleck
scatter plot representing percent growth inhibition of WT L. monocytogenes in the presence of a combination of a sublethal dose (1 μg/ml) of the β-lactam ceftriaxone and each compound in the screen. The solid black line represents the library mean (μ), and the dashed black line and gray line represent two (2σ) and three (3σ) S.D. above the library mean, respectively. The cyan, green, and red data points represent staurosporine, GSK690693, and other compounds from the IPA family, respectively.
J Biol Chem, 2017, 292(41):17037-17045. purchased from Selleck
(A) HTS assay timeline. Vero cells were seeded at a density of 1 × 104 cells per well in 96-well plates. After overnight incubation, cells were treated in duplicate with 10 μM compounds. One hour later, 20 μl RVPs was added. The supernatant was removed 1 h later and the compounds were readded to the cells for an additional 23 h. (B) (Left) HTS assay flowchart. The criterion required for the compounds to pass the primary screen was inhibition of >90%, and 28 primary candidates were selected. In the reconfirmation screen, 9 compounds with dose-dependent inhibition and cell viability of >80% were selected. (Middle) HTS of a library of 1,018 FDA-approved drugs for primary candidates inhibiting JEV infection. Each dot represents the percent inhibition achieved with each compound at a concentration of 10 μM. The dots located in the blue box represent inhibition of >90%. (Right) IC50s, CC50s, and SIs of nine compounds selected from the reconfirmation screen. The top five compounds depicted in the blue box showed SIs of greater than 10 and were designated hit drugs.
J Virol, 2017, e01055-17. purchased from Selleck
Normalized effect of inhibitors grouped according to their primary targets on SmoIP fluorescence. Effect of Hh stimulation on untreated cells set as 100% (dashed line). Diameter of circle reflects number of components per cluster, cutoff N ≥ 3, clusters sorted along X axis accordingly. Inhibitors used at 15 μM.
Sci Rep, 2017, 7(1):14341. purchased from Selleck
Select statin class drugs lysed S. mutans in an AK assay screen of the Selleck library. Statins were identified in the screening of the Selleck library against planktonic cultures of S. mutans UA159. The data are representative of 2 independent screens.
Antimicrob Agents Chemother, 2017, e01674-17. purchased from Selleck
• A unique collection of 29 small molecules affecting the development of diabetes.
• Targets including both type 1 and type 2 diabetes modulators: DPP-4, GPR, Potassium Channel, PPAR, SGLT, etc.
• Structurally diverse, medicinally active, and cell permeable.
• Rich documentation with structure and customer reviews.
• NMR and HPLC validated to ensure high purity.
|配制:||A unique collection of 29 anti-diabetes compounds supplied as pre-dissolved DMSO solutions|
|容器:||96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode|