ulk1

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.

MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.

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.

GW406108X(Z/E) is a mixture of different configurations of GW406108X, which is an inhibitor of Kinesin-12 and ULK1 .

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

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.

Ginkgolide K induces protective autophagy through the AMPK mTOR ULK1 signalling pathway. It possesses neuroprotective activity.

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.

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

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

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

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

DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. This capability positions DB1113 as a valuable tool for research into diseases or disorders associated with aberrant kinase activity [1].

(Rac)-BL-918 is the racemate of BL-918, a potent activator of UNC-51-like kinase 1 (ULK1) with an EC50 of 24.14 nM, inducing cytoprotective autophagy for Parkinson’s disease treatment [1].

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

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.

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

DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in research on diseases or disorders caused by aberrant kinase activity [1].

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

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).

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.

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).

AP39 free base is a mitochondrial-targeted H(2)S donor that can improve the survival rate of porcine islets in culture. AP39 free base regulates mitophagy through the AMPK-ULK1-FUNDC1 pathway, inhibits cell pyroptosis, and improves doxorubicin-induced myocardial fibrosis.

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

FMF-06-098-1 is a multitargeted depressant that promotes the degradation of various kinases including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].

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].