XST-14

XST-14 is an inhibitor of unc-51-like autophagy activating kinase 1 (ULK1, IC50 = 13.6 nM). It is selective for ULK1 over anaplastic lymphoma kinase 2 (ALK2), p38alpha MAPK, TGF-beta receptor type 2 (TGFBR2), and MEK1 (IC50s = 183.8, 283.9, 809.3, and 721.8 nM, respectively) but does inhibit calcium/calmodulin-dependent kinase II (CaMKII) and ULK2 (IC50s = 66.3 and 70.9 nM, respectively). XST-14 (5 µM) induces apoptosis and autophagy and decreases invasion in HepG2 hepatocellular carcinoma cells. In vivo, XST-14, alone and in combination with sorafenib (Cay-10009644, Cay-35612), decreases tumor volume in a HepG2 mouse xenograft model. InChI: InChI=1S/C16H21NO4/c1-9(2)20-11-6-13-12(15(7-11)21-10(3)4)8-14(17-13)16(18)19-5/h6-10,17H,1-5H3 InChIKey: ZNFMBFABCSHXPM-UHFFFAOYSA-N SMILES: O=C(C1=CC2=C(N1)C=C(OC(C)C)C=C2OC(C)C)OC