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  3. BL-918

BL-918 

Cat. No.: HY-124729
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BL-918 (compound 33i) is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.

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

BL-918 Chemical Structure

BL-918 Chemical Structure

CAS No. : 2101517-69-3

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Description

BL-918 (compound 33i) is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment[1].

IC50 & Target[1]

ULK1

24.14 nM (EC50)

In Vitro

BL-918 (5 μM; for 24 hours) induces autophagy in Neuron-Like cells[1].
BL-918 (0.5-50 μM; for 24 hours) can partially reverse MPP+-induced cell death, which is determined by enhancing cell viability[1].
BL-918 (5 μM; for 6-36 hours) time-dependently elevates the expression levels of LC3-II, Beclin-1, and its phosphorylation status, whereas reduces the level of the selective autophagy substrate SQSTM1/p62. BL-918 elevates Ser317 and Ser555 phosphorylation of ULK1, as well as decreases Ser757 phosphorylation of ULK1[1].
BL-918 binds to ULK1 with a high binding affinity (KD=0.719 μM)[1].

Cell Autophagy Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 5 μM
Incubation Time: For 24 hours
Result: Induced Autophagy.

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 0.5, 5, 50 μM
Incubation Time: For 24 hours
Result: Could partially reverse MPP+-induced cell death, which was determined by enhancing cell viability.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 5 μM
Incubation Time: 6, 12, 24, 36 hours
Result: Time-dependently elevated the expression levels of LC3-II (a key marker of autophagy), Beclin-1, and its phosphorylation status, whereas reduced the level of the selective autophagy substrate SQSTM1/p62.
In Vivo

BL-918 (20, 40, or 80 mg/kg/day; oral gavage; began 2 days before the first injection of saline/MPTP and continuously maintained for 5 days after the last injection of saline/MPTP) attenuates the loss of DA and its metabolites. BL-918 obviously decreases the levels of dopamine (DA), 3,4-dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA)[1].

Animal Model: Male C57BL/6 mice (eight-week old) weighing between 20 and 25 g[1]
Dosage: 20, 40, or 80 mg/kg
Administration: Oral gavage; daily; began 2 days before the first injection of saline/MPTP and continuously maintained for 5 days after the last injection of saline/MPTP
Result: Attenuated the loss of DA and its metabolites.
Molecular Weight

533.44

Formula

C₂₃H₁₅F₈N₃OS

CAS No.

2101517-69-3

SMILES

O=C(NC1=CC=C(F)C=C1F)[[email protected]](NC(NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=S)C3=CC=CC=C3

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BL-918BL918BL 918ULKAutophagyUnc-51 like kinaseOrallyUNC-51-likekinasecytoprotectiveautophagicParkinson’sdiseaseInhibitorinhibitorinhibit

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