ULK1, a serine/threonine protein kinase, is an enzyme that in humans is encoded by the ULK1 gene. ULK1 is essential for the initial stages of autophagy. ULK1 is an important protein in autophagy. It is part of the ULK1-complex, which is needed in early steps of autophagosome biogenesis. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation.ULK2 is essential for astrocyte transformation and tumor growth. ULK2 also inhibits the growth of glioma cells, which requires autophagy induction as kinase mutant of ULK2 fails to induce autophagy and inhibit growth. ULK2 and its homologue ULK1 are only down-regulated in all grades of glioma. Thus these results altogether suggest that inhibition of autophagy by ULK1/2 down-regulation is essential for glioma development.
||MRT68921 is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
||SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .
||MRT68921 hydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
||LYN-1604 hydrochloride is a potent ULK1 agonist with an EC50 of 18.94 nM.
||LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM.
||SR-20295 (SR20295) is a novel potent ULK1 inhibitor with IC50 of 45 nM.
||MRT-68921 hydrochloride (MRT68921) is a potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively.
||A novel potent ULK1 inhibitor with IC50 of 11 nM..