Protease Inhibitor Library
A unique collection of 53 small molecule inhibitors used for chemical genomics, high-throughput screening (HTS), and high content screening (HCS).
You can select compounds, quantities, format (dry/solid or DMSO) and plate map to meet your specific requirement.
Protease Inhibitor Library Contents
Cited by 14 Publications
22 Customer Reviews
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
Description & Advantages
• A unique collection of 53small molecule inhibitors used for chemical genomics, high-throughput screening (HTS), and high content screening (HCS).
• Bioactivity and safety confirmed by preclinical research and clinical trials.
• Targets proteasome, HCV Protease, DPP-4, Caspase, MMP, Gamma-secretase, Beta Amyloid.
• Structurally diverse, medicinally active, and cell permeable.
• Rich documentation with structure, IC50, and customer reviews.
• NMR and HPLC validated to ensure high purity.
|Formulation:||A unique collection of 53 protease inhibitors supplied as pre-dissolved DMSO solutions|
|Container:||96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode|