ULK

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.

Targets for ULK

Products for ULK

Cat.No. Product Name Information
GC73892 DCC-3116 DCC-3116 is an orally active ULK1/2 inhibitor.
GC60891 GW406108X

GW108X
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
GC19236 LYN-1604 LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM.
GC36517 LYN-1604 hydrochloride LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
GC17136 MRT67307 A kinase inhibitor
GC14086 MRT68921 A dual autophagy kinase ULK1/2 inhibitor
GC36654 MRT68921 dihydrochloride MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
GC15654 SBI-0206965
SBI-0206965 , the pyrimidine derivative , is a highly selective kinase ULK1 inhibitor with an IC₅₀ value of 108nM.
GC34315 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor, with IC50 values of 1.6 nM and 30 nM for ULK1 and ULK2, respectively. ULK-101 suppresses autophagy and sensitizes cancer cells to nutrient stress.
GC62146 XST-14 XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.