ULK

亜型選択性的な製品

ULK製品

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  • ULK阻害剤 (9)
  • ULK活性剤(1)
  • ULK作動薬(1)
  • 新製品
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S1092 KU-55933 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.
Nucleic Acids Res, 2024, gkad1224
Cell Rep Med, 2024, 5(2):101393
Clin Cancer Res, 2024, 30(1):187-197
S1113 GSK690693 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.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Cell Death Differ, 2024, 10.1038/s41418-024-01260-2
Cell Rep, 2024, 43(1):113575
PLoS Pathog, 2024, 20(1):e1011958
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Life Sci Alliance, 2023, 6(5)e202201605
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Commun, 2022, 13(1):6589
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Immunity, 2024, 57(2):287-302.e12
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
S8597 LYN-1604 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.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S6386 MRT67307 MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells.
Front Pharmacol, 2022, 13:924523
Microbiol Spectr, 2022, e0219321
E1750New XST-14 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. XST-14 reduces the phosphorylation of the ULK1 downstream substrate and induces autophagy inhibition. It exhibits antitumor effects.
E2012 Ginkgolide K Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway, and possesses neuroprotective activity.
S0819 BL-918 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. BL-918 induces cytoprotective autophagy for Parkinson's disease treatment.
S3393 SBP-7455 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.
S8597 LYN-1604 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.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S1092 KU-55933 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.
Nucleic Acids Res, 2024, gkad1224
Cell Rep Med, 2024, 5(2):101393
Clin Cancer Res, 2024, 30(1):187-197
S1113 GSK690693 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.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Cell Death Differ, 2024, 10.1038/s41418-024-01260-2
Cell Rep, 2024, 43(1):113575
PLoS Pathog, 2024, 20(1):e1011958
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Life Sci Alliance, 2023, 6(5)e202201605
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Commun, 2022, 13(1):6589
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Immunity, 2024, 57(2):287-302.e12
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
S6386 MRT67307 MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells.
Front Pharmacol, 2022, 13:924523
Microbiol Spectr, 2022, e0219321
E1750New XST-14 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. XST-14 reduces the phosphorylation of the ULK1 downstream substrate and induces autophagy inhibition. It exhibits antitumor effects.
S3393 SBP-7455 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.
S0819 BL-918 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. BL-918 induces cytoprotective autophagy for Parkinson's disease treatment.
S8597 LYN-1604 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.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
E1750New XST-14 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. XST-14 reduces the phosphorylation of the ULK1 downstream substrate and induces autophagy inhibition. It exhibits antitumor effects.

ULK阻害剤の選択性比較

Tags: ULK inhibitor|ULK agonist|ULK activator|ULK inducer|ULK antagonist|ULK signaling pathway|ULK assay kit