P-gp inhibitor 5 

P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In^TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015)^[1].

P-gp^[1]

P-gp inhibitor 5 (compound 10) has cytotoxic against ABCB1/Flp-In^TM-293 and KBvin cells with IC₅₀s of 29.7 and 12.6 μM, respectively^[1].
P-gp inhibitor 5 (2.5 and 5 μM) lows the IC₅₀s of KBvin cells for Vincristine to 7.59~36.82 nM, for Paclitaxel to 21.0~79.5 nM, for Doxorubicin to 85.7~111 nM; lows the IC₅₀s of HeLaS3 cells for Vincristine to 2.24~3.91 nM, for Paclitaxel to 8.81~9.58 nM, for Doxorubicin to 102~1260 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

517.98

C₂₈H₂₀ClNO₅S

2451298-06-7

O=C(NC1=C(C2=CC=CS2)C3=C(OC(C)=O)C=C(C4=CC=C(OC)C=C4)C=C3O1)C5=CC=CC=C5Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hung CC, et al. Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. Eur J Med Chem. 2020 Sep 1;201:112422.  [Content Brief]