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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).

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 activator of ULK1, 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.

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

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

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

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.

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.

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

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.

XST-14 is a competitive and specific inhibitor of ULK1 (IC50: 26.6 nM).XST-14 blocks autophagy by inhibiting the phosphorylation of ULK1 downstream substrates.XST-14 induces apoptosis and inhibits the growth of HCC cells.

Hydroxyprogesterone caproate (Delalutin) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.

DCC-3116 is an orally active, selective and potent ULK1/2 inhibitor with anticancer activity.DCC-3116 inhibits autophagy and can be used in cancer research.

SBP-1750 is a potent, orally active autophagy inhibitor with a dual mechanism of action. It functions as a kinase inhibitor, strongly suppressing ULK1 (IC50 = 8 nM) and ULK2 (IC50 = 50 nM) activity, while simultaneously inducing the degradation of ATG13 (EC50 = 114 nM). This dual-targeting approach effectively blocks autophagic flux and induces cell death, exhibiting significant efficacy particularly against KRAS-mutant cancers such as pancreatic and lung cancers.

SR-17398 is an inhibitor of Unc-51-Like Kinase 1 (ULK1) (IC50 = 22.4 uM).

LYN-1604 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).

MRT67307 is a kinase inhibitor of TBK1, MARK1-4, IKKε, and NUAK1 (IC50: 19, 27-52, 160, and 230 nM, respectively).

MRT68921 hydrochloride is a potent inhibitor of both ULK1 and ULK2 [IC50s: 2.9 and 1.1 nM, respectively].

HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).

MR-2088 is a selective inhibitor of ULK1 and ULK2, with pEC50 values of 8.3 and 8.7, respectively. It effectively inhibits autophagy by targeting ULK1/2-mediated pathways [1].

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.