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  4. BL-918

BL-918 

Cat. No.: HY-124729 Purity: 99.98%
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BL-918 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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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

BL-918 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)

ULK1

0.719 μM (Kd)

In Vitro

BL-918 (compound 33i) binds to ULK1 with a high binding affinity (KD=0.719 μM)[1].
BL-918 (5 μM; for 24 hours) induces autophagy in Neuron-Like SH-SY5Y 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].

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

BL-918 Related Antibodies

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 (compound 33i; 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].

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

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

Appearance

Solid

Formula

C23H15F8N3OS
CAS No.
SMILES

O=C(NC1=CC=C(F)C=C1F)[C@H](NC(NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=S)C3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (468.66 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8746 mL 9.3731 mL 18.7463 mL
5 mM 0.3749 mL 1.8746 mL 3.7492 mL
10 mM 0.1875 mL 0.9373 mL 1.8746 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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BL-918 Related Classifications

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.

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Keywords:

BL-9182101517-69-3BL918BL 918ULKAutophagyUnc-51 like kinaseOrallyUNC-51-likekinasecytoprotectiveautophagicParkinson’sdiseaseInhibitorinhibitorinhibit

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