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Cat. No.: HY-181804

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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.

For research use only. We do not sell to patients.

Formula: C₃₆H₂₈ClF₂N₉O₃
Molecular Weight:708.12

Storage:

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

MRS8288 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

In Vitro

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. Further protocols information, click here.

Chemical Information

Molecular Weight 708.12
Formula C₃₆H₂₈ClF₂N₉O₃
SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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