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SBP-7455 potently inhibited ULK1 2 enzymatic activity in vitro and in cells, reduced the viability of TNBC cells and had oral bioavailability in mice.

Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).

BL-918 is a potent activator of UNC-51-like kinase 1 (ULK1) with an EC50 of 24.14 nM.

ULK-101 is a potent and selective inhibitor of ULK1 (IC50s: 8.3 30 nM for ULK1 ULK2). It can suppress autophagy.

ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.ULK1-IN-2 has high cytotoxicity against cancer cells, with an IC50 value of 1.94 μM against A549 cells.ULK1-IN-2 can be used for the study of non-small-cell lung cancer.

ULK1-IN-3 (Compound 8) is a novel chalcone-based potential ULK1 inhibitor. This compound inhibits the cell cycle, autophagy, and induces apoptosis and oxidative stress in colorectal cancer cell lines.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

SBI-0206965 is a potent, selective, and cell-permeable autophagy kinase ULK1 inhibitor with an IC50 of 108 nM for ULK1 kinase activity and 711 nM for ULK2.

LYN-1604 is a novel ULK1 activator.It inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis.

MRT68921 is a potent and dual autophagy kinase ULK1 2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.

LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis.

GW406108X (GW108X) is a Kif15 inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X is also an ULK1 kinase inhibitor with pIC50 values of 6.37 (427 nM) and block autophagic flux.

MRT68921 dihydrochloride is a potent ULK1 and ULK2 inhibitor (IC50 of 2.9 nM and 1.1 nM, respectively).

HMS607P03 is an activator of SIRT1 which induces autophagic cell death via the AMPK-mTOR-ULK complex and induces mitophagy by the SIRT1-PINK1-Parkin pathway. HMS607P03 downregulates 14-3-3γ, catalase, profilin-1, and HSP90α.