SBP-5147
SBP-5147 is an orally active ULK1/ULK2 inhibitor, with an IC50 of 2 nM against ULK1 and an IC50 of 53 nM against ULK2. SBP-5147 inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagy flux, downregulates the expression of ATG13 and ATG101, upregulates the expression of MHC-I, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. SBP-5147 is applicable to research related to non-small cell lung cancer[1].
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- CAS 番号: 1884222-37-0
- 分子式: C17H18F3N5
- 分子量:349.35
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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ULK2 53 nM (IC50) |
ULK1 2 nM (IC50) |
SBP-5147 (Compound 5) binds to intracellular ULK1 in HEK293T cells in NanoBRET assays, with an IC50 of 47 nM[1].
SBP-5147 (10 μM; 1 h) inhibits the phosphorylation levels of ULK1 downstream substrates Beclin-1 (Ser15) and Vps34 (Ser249) by approximately 80% in transfected HEK293T cells[1].
SBP-5147 (10 μM; 18 h) inhibits autophagic flux in A549 cells under nutrient starvation and reduces the population of cells with high autophagic flux[1].
SBP-5147 (72 h) reduces the viability of A549, HCC827, H1373 and H1975 cells, with IC50 values of 91, 49, 40 and 35 nM, respectively[1].
SBP-5147 (1 μM; 8-24 h) induces caspase-dependent apoptosis in A549 cells[1].
SBP-5147 (15-30 nM; 72 h) significantly upregulates the expression of total MHC-I protein in H1373, HCC827 and A549 cells[1].
SBP-5147 potently inhibits ULK1 kinase activity (IC50 = 2 nM) and ULK2 kinase activity (IC50 = 53 nM) in biochemical ADP-Glo assays[2].
SBP-5147 (48 h) induces the degradation of ATG13 in A549 non-small cell lung cancer (NSCLC) cells, with an IC50 of 4.5 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells transfected with Myc-tagged WT ULK1 and Flag-tagged Beclin-1 or Vps34
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Concentration:10 μM
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Incubation Time:1 h
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Result:Inhibited phosphorylation of Beclin-1 at Ser15 by roughly 80% relative to DMSO-treated cells.
Inhibited phosphorylation of Vps34 at Ser249 by roughly 80% relative to DMSO-treated cells.
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Cell Line:A549 NSCLC cells expressing mCherry-GFP-LC3 reporter
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Concentration:10 μM
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Incubation Time:18 h
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Result:Reduced the percentage of cells exhibiting high autophagic flux, shifting populations to intermediate and low flux relative to EBSS-only treated cells.
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Cell Line:A549, H1975 NSCLC cells
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Concentration:1 μM
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Incubation Time:24 h (imaging); 8 h (Western blot)
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Result:Induced caspase-dependent apoptotic cell death in A549 cells, with cell death abrogated by Emricasan and partially inhibited by zVAD-fmk.
Induced cleavage of PARP and caspase-3, blocked by apoptosis inhibitors.
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Cell Line:H1373, HCC827, A549, H1975 NSCLC cell lines
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Concentration:15 nM, 30 nM
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Incubation Time:72 h
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Result:Significantly increased total MHC-I protein expression at 30 nM in H1373, HCC827, and A549 cells.
Increased expression in H1373 and HCC827 cells also at 15 nM.
Had no significant effect on H1975 cells.
| Species | Dose | Route | Tmax | Cmax | T1/2 |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 0.25 h | 664 nM | 2.5 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (8-week-old female)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Caused progressive, significant decrease in ATG13 and ATG101 protein levels in liver and lung tissues.
Maintained significantly reduced ATG13 and ATG101 levels at 24 hours postdosing (plasma SBP-5147 almost completely eliminated) compared to vehicle-treated samples.
Confirmed statistically significant reductions in both proteins at 4, 8, and 24 hours postdosing relative to vehicle controls.
化学情報
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CAS 番号 1884222-37-0
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分子量 349.35
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分子式 C17H18F3N5
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SMILES
FC(F)(F)C1=C(NC2CC2)N=C(NC3=CC(CCNC4)=C4C=C3)N=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Layng FIAL, et al. Synthesis and Characterization of ULK1/2 Kinase Inhibitors That Inhibit Autophagy and Upregulate Expression of Major Histocompatibility Complex I for the Treatment of Non-Small Cell Lung Cancer. ACS Chem Biol. 2026 Feb 12. [Content Brief]
[2]. Hagan PM, et al. ULK1/2 Inhibitors that Degrade ATG13 Effectively Target KRAS-Mutant Cancers. bioRxiv [Preprint]. 2025 Oct 15:2025.10.14.682402. [Content Brief]
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