| S7949 |
MRT68921 HCl
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MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
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Autophagy, 2025, 1-20.
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Theranostics, 2025, 15(1):258-276
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EMBO Mol Med, 2025, 17(12):3472-3495
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| S7885 |
SBI-0206965
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SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. This compound inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
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Cell Res, 2025, 10.1038/s41422-025-01085-9
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Theranostics, 2025, 15(1):258-276
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Cell, 2024, 187(15):4043-4060.e30
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| S8793 |
ULK-101
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ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
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Theranostics, 2025, 15(1):258-276
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Immunity, 2024, 57(2):287-302.e12
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Cell Rep, 2024, 43(1):113575
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| S8597 |
LYN-1604
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LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
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Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
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J Virol, 2021, JVI0155021
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Exp Eye Res, 2019, 184:126-134
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| E1750 |
XST-14
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XST-14 is a potent, competitive, and highly selective inhibitor of ULK1 and exhibits an IC50 of 26.6 nM in an in vitro ULK1 kinase activity assay, respectively. This compound reduces the phosphorylation of the ULK1 downstream substrate and induces autophagy inhibition. It exhibits antitumor effects.
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| S0819 |
BL-918
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BL-918 is a potent, orally active activator of UNC-51-like kinase 1 (ULK1) with EC50 of 24.14 nM and Kd of 0.719 μM. This compound induces cytoprotective autophagy for Parkinson's disease treatment.
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| S3393 |
SBP-7455
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SBP-7455 is a dual-Specific ULK1/2 autophagy inhibitor with IC50s of 13 nM and 476 nM for ULK1 and ULK2 in ADP-Glo assay, respectively.
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| E1954New |
DCC-3116
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DCC-3116 is a selective inhibitor of ULK1/2 that blocks both basal and sotorasib-induced autophagy in KRAS G12C-driven cell lines and exhibits anti-tumor activity.
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| S1092 |
KU-55933
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KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
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Nature, 2025, 646(8086):992-1000
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Nat Cell Biol, 2025, 27(10):1771-1784
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Nat Commun, 2025, 16(1):8476
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| S1113 |
GSK690693
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GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
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Theranostics, 2025, 15(18):9819-9837
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Cell Rep, 2025, 44(7):115947
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Front Cell Infect Microbiol, 2025, 15:1543186
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