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Selleck Chemicals z fa fmk

Prediction dataset validation with a cell-free CTSL activity detection system. A, Among the available molecules, the top 50 molecules from the prediction dataset were chosen for verifying the inhibition effect against CTSL in a cell-free system at a single dose of 100 μM. Twelve of the 50 predicted molecules displayed over 50% inhibition against CTSL, and the top 5 were Mg-132, <t>Z-FA-FMK,</t> <t>leupeptin</t> hemisulfate, Mg-101 and calpeptin, with inhibition efficiencies greater than 90%. The data are expressed as the mean of three individual trials. B-F, Five predicted CTSL inhibitors, Mg-132(B), Z-FA-FMK(C), leupeptin hemisulfate(D), Mg-101(E) and calpeptin(F), with inhibition efficiencies greater than 90% at 100 μM were further tested for determination of the half maximal inhibitory concentration (IC 50 ) in the cell-free system. Corresponding molecular structure was drawn by Chemdraw. Non-linear fit to a variable response curve from one representative experiment with three replicates is shown (black lines). The data are expressed as the mean ± s.e.m.

Z Fa Fmk, supplied by Selleck Chemicals, used in various techniques. Bioz Stars score: 93/100, based on 11 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/fa/Z-FA-FMK/pmc09110316-69-4-37
Average 93 stars, based on 11 article reviews

z fa fmk - by Bioz Stars, 2026-11

93/100 stars

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1) Product Images from "Potential Drug Discovery for COVID-19 Treatment Targeting Cathepsin L Using a Deep Learning-Based Strategy"

Article Title: Potential Drug Discovery for COVID-19 Treatment Targeting Cathepsin L Using a Deep Learning-Based Strategy

Journal: Computational and Structural Biotechnology Journal

doi: 10.1016/j.csbj.2022.05.023

Figure Legend Snippet: Prediction dataset validation with a cell-free CTSL activity detection system. A, Among the available molecules, the top 50 molecules from the prediction dataset were chosen for verifying the inhibition effect against CTSL in a cell-free system at a single dose of 100 μM. Twelve of the 50 predicted molecules displayed over 50% inhibition against CTSL, and the top 5 were Mg-132, Z-FA-FMK, leupeptin hemisulfate, Mg-101 and calpeptin, with inhibition efficiencies greater than 90%. The data are expressed as the mean of three individual trials. B-F, Five predicted CTSL inhibitors, Mg-132(B), Z-FA-FMK(C), leupeptin hemisulfate(D), Mg-101(E) and calpeptin(F), with inhibition efficiencies greater than 90% at 100 μM were further tested for determination of the half maximal inhibitory concentration (IC 50 ) in the cell-free system. Corresponding molecular structure was drawn by Chemdraw. Non-linear fit to a variable response curve from one representative experiment with three replicates is shown (black lines). The data are expressed as the mean ± s.e.m.

Techniques Used: Activity Assay, Inhibition, Concentration Assay

The predicted CTSL inhibitors from bioactive compounds prevent SARS-CoV-2 pseudovirus infection in Huh7 cells in vitro. A, Schematic of the predicted CTSL inhibitor assay setup. Huh7 cells were pretreated with different drugs 1 hour(h) before infection with SARS-CoV-2 pseudovirus or SARS-CoV-2 B.1.351 (Beta) variant pseudovirus at the same dose (1.3×10 4 TCID 50 /ml). Pseudovirus infection and cell viability were evaluated 24 h later by a luciferase activity and MTT assay, respectively. B-F, Inhibition of pseudovirus infection by different doses of Mg-132 (B), Z-FA-FMK (C), Leupeptin Hemisulfate (D), Mg-101 (E), and Calpeptin (F) and viability of Huh7 cells treated with different doses of the drugs as indicated. Non-linear fit to a variable response curve from one representative experiment with four replicates is shown (red lines). Cytotoxic effect on Huh7 cells exposed to increasing concentrations of drugs in the absence of virus is also shown (blue lines). The CC 50 , EC 50 , and SI values of this graph are indicated. n=4. The data are expressed as the mean ± s.e.m. G-K, Inhibition of SARS-CoV-2 B.1.351(Bata) variant pseudovirus infection by different doses of Mg-132 (G), Z-FA-FMK (H), Leupeptin Hemisulfate (I), Mg-101 (J), and Calpeptin (K) and viability of Huh7 cells treated with different doses of the drugs as indicated. Non-linear fit to a variable response curve from one representative experiment with four replicates is shown (purple lines). Cytotoxic effect on Huh7 cells exposed to increasing concentrations of drugs in the absence of virus is also shown (blue lines). The CC 50 , EC 50 , and SI values of this graph are indicated. CC 50 : 50% cytotoxic concentration. EC 50 : half maximal effective concentration. SI: the selectivity index, which is calculated as the ratio of CC 50 and EC 50 . n=4. The data are expressed as the mean ± s.e.m.

Figure Legend Snippet: The predicted CTSL inhibitors from bioactive compounds prevent SARS-CoV-2 pseudovirus infection in Huh7 cells in vitro. A, Schematic of the predicted CTSL inhibitor assay setup. Huh7 cells were pretreated with different drugs 1 hour(h) before infection with SARS-CoV-2 pseudovirus or SARS-CoV-2 B.1.351 (Beta) variant pseudovirus at the same dose (1.3×10 4 TCID 50 /ml). Pseudovirus infection and cell viability were evaluated 24 h later by a luciferase activity and MTT assay, respectively. B-F, Inhibition of pseudovirus infection by different doses of Mg-132 (B), Z-FA-FMK (C), Leupeptin Hemisulfate (D), Mg-101 (E), and Calpeptin (F) and viability of Huh7 cells treated with different doses of the drugs as indicated. Non-linear fit to a variable response curve from one representative experiment with four replicates is shown (red lines). Cytotoxic effect on Huh7 cells exposed to increasing concentrations of drugs in the absence of virus is also shown (blue lines). The CC 50 , EC 50 , and SI values of this graph are indicated. n=4. The data are expressed as the mean ± s.e.m. G-K, Inhibition of SARS-CoV-2 B.1.351(Bata) variant pseudovirus infection by different doses of Mg-132 (G), Z-FA-FMK (H), Leupeptin Hemisulfate (I), Mg-101 (J), and Calpeptin (K) and viability of Huh7 cells treated with different doses of the drugs as indicated. Non-linear fit to a variable response curve from one representative experiment with four replicates is shown (purple lines). Cytotoxic effect on Huh7 cells exposed to increasing concentrations of drugs in the absence of virus is also shown (blue lines). The CC 50 , EC 50 , and SI values of this graph are indicated. CC 50 : 50% cytotoxic concentration. EC 50 : half maximal effective concentration. SI: the selectivity index, which is calculated as the ratio of CC 50 and EC 50 . n=4. The data are expressed as the mean ± s.e.m.

Techniques Used: Infection, In Vitro, Variant Assay, Luciferase, Activity Assay, MTT Assay, Inhibition, Concentration Assay

The predicted CTSL inhibitors from bioactive compounds prevent live SARS-CoV-2 infection in Huh7 cells in vitro. A, Schematic of the predicted CTSL inhibitor assay setup. Huh7 cells were pretreated with different drugs 1 h before infection with live SARS-CoV-2 at the same dose (0.5 moi), followed by changing to fresh medium with the indicated concentrations of drugs 1 h later. The detection of infected cells was performed 48 h later by using an immunofluorescence assay. B-D, Inhibition of live SARS-CoV-2 infection by different doses of Mg-132 (B), Z-FA-FMK (C), and Leupeptin Hemisulfate (D). Non-linear fit to a variable response curve from one representative experiment with three replicates is shown (blue lines). The EC 50 value of this graph is indicated. n = 3. The data are expressed as the mean ± s.e.m.

Figure Legend Snippet: The predicted CTSL inhibitors from bioactive compounds prevent live SARS-CoV-2 infection in Huh7 cells in vitro. A, Schematic of the predicted CTSL inhibitor assay setup. Huh7 cells were pretreated with different drugs 1 h before infection with live SARS-CoV-2 at the same dose (0.5 moi), followed by changing to fresh medium with the indicated concentrations of drugs 1 h later. The detection of infected cells was performed 48 h later by using an immunofluorescence assay. B-D, Inhibition of live SARS-CoV-2 infection by different doses of Mg-132 (B), Z-FA-FMK (C), and Leupeptin Hemisulfate (D). Non-linear fit to a variable response curve from one representative experiment with three replicates is shown (blue lines). The EC 50 value of this graph is indicated. n = 3. The data are expressed as the mean ± s.e.m.

Techniques Used: Infection, In Vitro, Immunofluorescence, Inhibition

Molecular docking results of CTSL inhibitors in the crystal structure of human CTSL (5MQY). A-G, 3D structure of the human CTSL (5MQY) showing the main residues involved in the protein-ligand interaction of Compound 35 (A), Mg-132 (B), Z-FA-FMK (C), Leupeptin Hemisulfate (D), Calpeptin (E), Mg-101 (F) and Daptomycin (G). Compound 35 is a covalent inhibitor cocrystallized with human CTSL protein in 5MQY, used here as a positive control. Short intermolecular contacts with distances of < 4.0 Å between the ligand fragment (gray) and protein residues (dark green) are shown as dashed yellow lines. Structure visualization was by PyMol.

Figure Legend Snippet: Molecular docking results of CTSL inhibitors in the crystal structure of human CTSL (5MQY). A-G, 3D structure of the human CTSL (5MQY) showing the main residues involved in the protein-ligand interaction of Compound 35 (A), Mg-132 (B), Z-FA-FMK (C), Leupeptin Hemisulfate (D), Calpeptin (E), Mg-101 (F) and Daptomycin (G). Compound 35 is a covalent inhibitor cocrystallized with human CTSL protein in 5MQY, used here as a positive control. Short intermolecular contacts with distances of < 4.0 Å between the ligand fragment (gray) and protein residues (dark green) are shown as dashed yellow lines. Structure visualization was by PyMol.

Techniques Used: Positive Control

other:

Article Title: Pharmacological targeting of TFIIH suppresses KRAS mutant pancreatic ductal adenocarcinoma and synergizes with TRAIL
Article Snippet: For immunoblotting, unless otherwise indicated, all antibodies listed with only catalog numbers were obtained from Cell Signaling Technology: CFLAR (ALX-804-961 ENZO), Rb (554136 BD Pharmingen), Caspase-8 (9746), Caspase-3 (9665), Mcl-1 (sc-12756), PARP (9542), XIAP (2042), Bcl-xL (2764), Cleaved Caspase-3 (9664), p53 Ab-5 (DO-7) (MS-186-P ThermoFisher Scientific, p53 (DO-7) (MA5-12557 Thermofisher Scientific), Phospho-Histone H2A.X (9718), Phospho-Rb (Ser608) (2181), p21 (556430 BD Pharmingen), c-MYC (61075-Active Motif), GAPDH (5174), cdc2 (CDK1) (9116), XPB (8746), XPD (11963), CDK2 (2546), Phospho-cdc2 (CDK1) (Thr161) (9114), Phospho-CDK2 (Thr160) (2561), Cleaved PARP (9546), Anti-RNA polymerase II subunit B1 (phospho-CTD Ser-2) clone 3E1 (04-1571-I Millipore), RNA pol II CTD phospho-Ser5 (61701-Active Motif), RPB1/Pol II (A-10) (sc-17798 Santa Cruz), TRAIL R1/TNFRSF10A (NB100-56747 Novusbio), TRAIL R2/TNFRSF10B (NB100-56618 Novusbio), MEK1/2 (4694), Phospho-MEK1/2 (Ser217/221) (9154), RAS (ab55391 Abcam), SMAD4 (sc-7966 Santa Cruz), AKT (pan) (4691), Beta-Actin (3598R-100 Biovision), STAT3 (9139), FOSL1 (5281), FOSL2 (19967), and E2F1 (3742).

Control:

Article Title: Pharmacological targeting of TFIIH suppresses KRAS mutant pancreatic ductal adenocarcinoma and synergizes with TRAIL
Article Snippet: .. Cell lines were treated with vehicle (DMSO) and 500nM THZ1, 500nM SNS-032, and 500nM Triptolide with and without a cysteine protease/effector caspase inhibitor as a control (Z-FA-FMK) (S7391 Selleckchem) and a specific caspase-8 inhibitor (Z-IETD-FMK) (S7314 Selleckchem) for 24 hrs in a 37°C incubator at 5%CO2 in air. .. Raw luminescence signals were measured with the CellTiterGlo assay (Promega) utilizing a Synergy H4 (Biotek).

Protease Inhibitor:

Article Title: Nucleic acid stabilization reagent, kits, and methods of use thereof
Article Snippet: .. A cysteine protease inhibitor may be, but is not limited to any of E-64 (N-(trans-epoxysuccinyl)-L-leucine-4-guanidinobutylamide, Selleck Chem), N-benzoyl phenylalanine fluoromethyl ketone (Z-FA-FMK), and N-benzoyl valinyl alaninyl aspartic fluoromethyl ketone (Z-VAD-FMK). ..

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