MBL-II-141

MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562) ) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM) . MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers[1][2].

Product Specifications

CAS Number

[1353747-12-2]

UNSPSC

12352005

Target

BCRP

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(C1=CC(C2=C(OCC3=CC=C(Br)C=C3)C=CC=C2O1)=O)NCCC4=CNC5=C4C=C(OC)C=C5

Molecular Formula

C28H23BrN2O5

Molecular Weight

547.40

References & Citations

[1]Hénin E, et al. Pharmacokinetic interactions in mice between irinotecan and MBL-II-141, an ABCG2 inhibitor. Biopharm Drug Dispos. 2017 Jul;38 (5) :351-362.|[2]Payen L, et al. MBL-II-141, a chromone derivative, enhances irinotecan (CPT-11) anticancer efficiency in ABCG2-positive xenografts. Oncotarget. 2014 Dec 15;5 (23) :11957-70.