A dual inhibitor of ULK1 and ULK2
SBP-7455 is a dual inhibitor of unc-51-like autophagy activating kinase 1 (ULK1) and ULK2 (IC50s = 13 and 476 nM, respectively, for the recombinant human enzymes in cell-free assays).1 It inhibits increases in autophagic flux and induces apoptosis in serum-deprived MDA-MB-468 breast cancer cells when used at a concentration of 10 µM. SBP-7455 (0.19 µM), alone or in combination with olaparib , reduces the viability of MDA-MB-468 cells.
1.Ren, H., Bakas, N.A., Vamos, M., et al.Design, synthesis, and characterization of an orally active dual-specific ULK1/2 autophagy inhibitor that synergizes with the PARP inhibitor olaparib for the treatment of triple-negative breast cancerJ. Med. Chem.63(23)14609-14625(2020)
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