CYP51/SE-IN-1
CYP51/SE-IN-1 is a dual-target inhibitor of CYP51 and squalene epoxidase (SE), with IC50 values of 2.95 mg/L and 6.35 mg/L, respectively. CYP51/SE-IN-1 is also an Antifungal agent. CYP51/SE-IN-1 disrupts fungal cell membrane integrity, increases membrane permeability, and induces intracellular ROS accumulation. CYP51/SE-IN-1 inhibits ergosterol biosynthesis and exhibits broad-spectrum antifungal activity against plant pathogenic fungi.
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- Formule: C21H21F5N4O
- Masse moléculaire:440.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
CYP51 2.95 μg/mL (IC50) |
In Vitro
CYP51/SE-IN-1 (Compound 6o) (10 mg/L) exhibited broad-spectrum antifungal activity against V. mali, S. sclerotiorum, R. solani, C. lunata, and B. cinerea, with the highest potency against V. mali (EC50 = 0.25 mg/L)[1].
CYP51/SE-IN-1 (5-10 mg/L; 30-210 min) increases the cell membrane permeability of V. mali mycelia in a time- and concentration-dependent manner[1].
CYP51/SE-IN-1 (5-10 mg/L) inhibits ergosterol biosynthesis in V. mali, reaching an inhibition rate of 59.94% at 10 mg/L[1].
CYP51/SE-IN-1 (0.25-0.5 mg/L) induces oxidative stress by elevating intracellular ROS levels and causes damage to the cell membrane of V. mali[1].
CYP51/SE-IN-1 is a dual inhibitor of CYP51 (IC50 = 2.95 mg/L) and SE (IC50 = 6.35 mg/L)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Masse moléculaire 440.41
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Formule C21H21F5N4O
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SMILES
OC(CN1N=CN=C1)(C2=CC=C(F)C=C2F)CN(CC)CC3=CC=C(C(F)(F)F)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)