P-gp inhibitor 5

Names

[ CAS No. ]:
2451298-06-7

[ Name ]:
P-gp inhibitor 5

Biological Activity

[Description]:

P-gp inhibitor 5 (compound 10) is a potent P-glycoprotein (P-gp) inhibitor with P-gp inhibition fold of 2.5 and 3.0 at 1.25 μM and 2.5 μM. 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-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine and Paclitaxel[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

[Target]

P-gp[1]


[In Vitro]

P-gp inhibitor 5 (compound 10) has cytotoxic against ABCB1/Flp-InTM-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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H20ClNO5S

[ Molecular Weight ]:
517.98


Related Compounds