CYP1B1-IN-15
CYP1B1-IN-15 is a CYP1B1 inhibitor with an IC50 of 1.47 nM, and it exhibits high selectivity against six major CYP subtypes. CYP1B1-IN-15 exerts competitive inhibitory effects by competing with substrates for binding to the active site of CYP1B1. CYP1B1-IN-15 enhances the inhibitory effect of Paclitaxel (HY-B0015) on the proliferation of paclitaxel-resistant cancer cells, and inhibits the migration and invasion of paclitaxel-resistant cancer cells. CYP1B1-IN-15 can be used in studies related to paclitaxel-resistant non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C18H11F2N3O2S
- Molecular Weight:371.36
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
CYP1B1 1.47 nM (IC50) |
CYP1A1 0.41 μM (IC50) |
CYP1A2 > 100 μM (IC50) |
CYP1B1-IN-15 (Compound C27) (10 μM; 48 h) exhibits low cytotoxicity toward normal BEAS-2B lung epithelial cells and A549 non-small cell lung cancer cells, and significantly inhibits the growth of paclitaxel-resistant A549/T cells at a concentration of 10 μM[1].
CYP1B1-IN-15 (10 μM; 48 h) significantly enhances the sensitivity of paclitaxel-resistant A549/T cells to paclitaxel, reducing the IC50 of paclitaxel by 4.8-fold at a concentration of 10 μM[1].
CYP1B1-IN-15 (2.5-10 μM; 14 days) inhibits the clonogenic capacity of paclitaxel-resistant A549/T cells in a dose-dependent manner[1].
CYP1B1-IN-15 (2.5-10 μM; 48 h) inhibits the migration of paclitaxel-resistant A549/T cells within 48 h in a dose-dependent manner[1].
CYP1B1-IN-15 (2.5-10 μM; 24 h) effectively inhibits the invasion of paclitaxel-resistant A549/T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549/Taxol cell
-
Concentration:10 μM
-
Incubation Time:48 h
-
Result:Reduced the paclitaxel IC50 in A549/T cells from 10.59 μM to 2.20 μM, representing a 4.8-fold reversal of paclitaxel resistance.
Showed concentration-dependent resistance reversal with increasing CYP1B1-IN-15 doses.
-
Cell Line:A549/Taxol cell
-
Concentration:2.5, 5 and 10 μM
-
Incubation Time:~14 days
-
Result:Inhibited A549/T cell colony formation in a dose-dependent manner, with significant reduction in colony numbers observed at 5.0 μM.
-
Cell Line:A549/Taxol cell
-
Concentration:2.5, 5 and 10 μM
-
Incubation Time:24 h
-
Result:Effectively blocked A549/T cell invasion at 5 μM, with an effect significantly superior to the positive control TMS.
Chemical Information
-
Molecular Weight 371.36
-
Formula C18H11F2N3O2S
-
SMILES
FC(F)OC(C=C1)=CC=C1NC(C2=CSC(C3=CC=C(C#N)C=C3)=N2)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)