P-gp/BCRP-IN-2

P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM) . P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells[1].

Product Specifications

UNSPSC

12352005

Target

BCRP; P-glycoprotein

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/p-gp-bcrp-in-2.html

Solubility

10 mM in DMSO

Smiles

COC1=CC(/C=C/C2=NN=C(O2)C(C=C3)=CC=C3CCN4CCC5=CC(OC)=C(OC)C=C5C4)=CC(OC)=C1OC

Molecular Formula

C32H35N3O6

Molecular Weight

557.64

References & Citations

[1]Braconi L, et al. Tetrazole and oxadiazole derivatives as bioisosteres of tariquidar and elacridar: New potent P-gp modulators acting as MDR reversers. Eur J Med Chem. 2023 Nov 5;259:115716..