MRS8288 

MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC₅₀ of 0.96 μM against ABCG2 and an IC₅₀ of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research^[1].

MRS8288 (20 min) potently inhibits the basal ATPase activity of P-glycoprotein derived from High-Five insect cells, with an IC₅₀ of 1.39±0.20 μM^[1].
MRS8288 (20 min) potently inhibits the basal ATPase activity of ABCG2 derived from High-Five insect cells, with an IC₅₀ of 0.96±0.15 μM^[1].
MRS8288 (0-10 μM) potently inhibits ABCG2-mediated transport of Mitoxantrone (HY-13502) and Pheophorbide A (HY-125665) in HEK293-R5 cells, with IC₅₀ values of 2.49±0.16 μM and 4.86±0.4 μM, respectively^[1].
MRS8288 (72 h) exhibits cytotoxicity against both HEK293-pcDNA control cells and HEK293-R5 cells expressing ABCG2, with IC₅₀ values of 5.19±0.1 μM and 4.06±0.6 μM, respectively^[1].

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

708.12

C₃₆H₂₈ClF₂N₉O₃

O[C@@H]1[C@H](O)[C@](C(NC)=O)(C2)[C@H]2[C@H]1N(C=N3)C4=C3C(NCC5=CC=CC(N6N=NC(C7=CC=C(C=C7)Cl)=C6)=C5)=NC(C#CC8=CC=C(C(F)=C8)F)=N4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Murakami M, et al. (N)-Methanocarba Adenosine Derivatives as Dual Modulators of P-Glycoprotein and ABCG2 Transporters. J Med Chem. 2026;69(4):4945-4968.  [Content Brief]