MR-2088 | ULK1/2 inhibitor | Probechem Biochemicals

Chemical Structure : MR-2088

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MR-2088 (MR2088, MR 2088)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	406.43
分子式	C19H17F3N4OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

MR-2088 (MR2088, MR 2088)

生物&药学活性

物理化学性质&存储条件

参考文献

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MR-2088 (MR2088, MR 2088)

生物&药学活性

物理化学性质&存储条件

参考文献

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