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MR-2088

Chemical Structure : MR-2088

CAS No.: 2922531-69-7

MR-2088 (MR2088, MR 2088)

Catalog No.: PC-21692Not For Human Use, Lab Use Only.

MR-2088 is a potent and selective ULK1/2 inhibitor with IC50 of 2.0 nM and MST Kd value of 1.5-4.4 nM (ULK1), efficiently inhibits autophagy.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MR-2088 is a potent and selective ULK1/2 inhibitor with IC50 of 2.0 nM and MST Kd value of 1.5-4.4 nM (ULK1), efficiently inhibits autophagy.
MR-2088 displays a relatively clean kinome-wide profile with an S (35) selectivity score of 0.295 against 97 diverse human kinases and disease-relevant mutants at 1 uM.
MR-2088 inhibits the phosphorylation of ATG13 Ser 318 and prevents the degradation of p62 with EC50 36 nM and 48 nM for inhibiting downstream phosphorylation of ATG13 under starved and trametinib-treated conditions, respectively.
MR-2088 blocks autophagy flux, exhibits synergistic antiproliferative activity with MEK inhibition.

Physicochemical Properties

M.Wt 406.43
Formula C19H17F3N4OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(2-(1,2,5,6-Tetrahydropyridin-3-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-N-(2,2,2-trifluoroethyl)thiophene-2-carboxamide

References

1. Alisa Morozova, et al. Eur J Med Chem. 2023 Dec 29:266:116101.

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