P-gp/BCRP-IN-2

P-gp/BCRP-IN-2

• UNSPSC Description: 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].
• Target Antigen: 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 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..
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported