ULK-100
ULK-100 is a potent ULK1/ULK2 inhibitor, with IC50 values of 1.6 nM and 2.6 nM against human ULK1 and ULK2, respectively. ULK-100 reduces ULK1-mediated phosphorylation of Beclin 1 at Ser15, inhibits autophagy by targeting the ULK1 pathway, and also suppresses autophagy in tumor cells. ULK-100 enhances the sensitivity of tumor cells to nutrient deprivation. ULK-100 can be used in research on autophagy initiation and cancer.
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- CAS No.: 945377-65-1
- Formule: C29H32F3N5O2S
- Masse moléculaire:571.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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ULK1 1.6 nM (IC50) |
ULK2 2.6 nM (IC50) |
ULK-100 directly inhibits human recombinant ULK1 and ULK2 in radiometric kinase assays, with IC50 values of 1.6 nM and 2.6 nM, respectively[1].
ULK-100 (0.06-1 μM; 1 h) dose-dependently inhibits ULK1-mediated phosphorylation of Beclin 1 Ser15 in 293FT cells expressing HA-hULK1, V5-Beclin 1 and EGFP-ATG14, with a cellular EC50 of 83 nM[1].
ULK-100 (15 nM) inhibits ULK1 activity by approximately 88% in a radiometric kinase panel containing 327 human kinases, while the inhibition level of 18 non-ULK1 kinases reaches at least 75% of that of ULK1, indicating its limited kinome selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293FT cells expressing HA-hULK1, V5-Beclin 1 and EGFP-ATG14
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Concentration:0.06, 0.13, 0.25, 0.5 and 1 μM
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Incubation Time:1 h
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Result:Dose-dependently reduced Beclin 1 Ser15 phosphorylation with a cellular EC50 of 83 nM.
Chemical Information
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CAS No. 945377-65-1
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Masse moléculaire 571.66
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Formule C29H32F3N5O2S
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SMILES
O=C(C1=CC(C2=C3N=CC(C4=CC=C(OCCN5CCCCC5)C=C4)=CN3N=C2)=CS1)N[C@@H](C(C)C)C(F)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Martin KR, et al. A Potent and Selective ULK1 Inhibitor Suppresses Autophagy and Sensitizes Cancer Cells to Nutrient Stress. iScience. 2018 Oct 26;8:74-84. [Content Brief]
[2]. Liu L, et al. A Review of ULK1-Mediated Autophagy in Drug Resistance of Cancer. Cancers. 2020 Feb 04;12(2):352. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ULK-100 Related Classifications
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