2. Autophagy Immunology/Inflammation Apoptosis
  3. ULK Beclin1 Autophagy MHC Caspase Apoptosis
  4. 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].

For research use only. We do not sell to patients.

SBP-5147

SBP-5147 Chemical Structure

CAS No. : 1884222-37-0

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SBP-5147 Related Antibodies

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ULK1 ULK2

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MHC I MHC II

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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][2].

IC50 & Target

ULK2

53 nM (IC50)

ULK1

2 nM (IC50)

In Vitro

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.

SBP-5147 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T cells transfected with Myc-tagged WT ULK1 and Flag-tagged Beclin-1 or Vps34
Concentration: 10 μM
Incubation Time: 1 h
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.

Cell Autophagy Assay[1]

Cell Line: A549 NSCLC cells expressing mCherry-GFP-LC3 reporter
Concentration: 10 μM
Incubation Time: 18 h
Result: Reduced the percentage of cells exhibiting high autophagic flux, shifting populations to intermediate and low flux relative to EBSS-only treated cells.

Apoptosis Analysis[1]

Cell Line: A549, H1975 NSCLC cells
Concentration: 1 μM
Incubation Time: 24 h (imaging); 8 h (Western blot)
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.

Western Blot Analysis[1]

Cell Line: H1373, HCC827, A549, H1975 NSCLC cell lines
Concentration: 15 nM, 30 nM
Incubation Time: 72 h
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.
Parmacokinetics
Species Dose Route Tmax Cmax T1/2
Mice[1] 10 mg/kg p.o. 0.25 h 664 nM 2.5 h
In Vivo

SBP-5147 (10 mg/kg; p.o.; single administration) reduces the protein levels of ATG13 and ATG101 in the liver and lung tissues of C57BL/6J mice, indicating that it can persistently target and inhibit autophagy[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (8-week-old female)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

349.35

Formula

C17H18F3N5
CAS No.
SMILES

FC(F)(F)C1=C(NC2CC2)N=C(NC3=CC(CCNC4)=C4C=C3)N=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SBP-5147 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SBP-51471884222-37-0SBP5147SBP 5147ULKBeclin1AutophagyMHCCaspaseApoptosisUnc-51 like kinaseAtg6Major Histocompatibility ComplexULK1/ULK2 inhibitorHEK293T cellsA549 cellsHCC827 cellsH1373 cellsH1975 cellsC57BL/6J miceautophagyapoptosisInhibitorinhibitorinhibit

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