2. Autophagy
  3. ULK Autophagy
  4. BL-918

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.

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BL-918 Chemical Structure

BL-918 Chemical Structure

CAS No. : 2101517-69-3

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Based on 1 publication(s) in Google Scholar

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BL-918 Related Antibodies

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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

Formula

C23H15F8N3OS
CAS No.
Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8746 mL 9.3731 mL 18.7463 mL 46.8656 mL
5 mM 0.3749 mL 1.8746 mL 3.7493 mL 9.3731 mL
10 mM 0.1875 mL 0.9373 mL 1.8746 mL 4.6866 mL
15 mM 0.1250 mL 0.6249 mL 1.2498 mL 3.1244 mL
20 mM 0.0937 mL 0.4687 mL 0.9373 mL 2.3433 mL
25 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8746 mL
30 mM 0.0625 mL 0.3124 mL 0.6249 mL 1.5622 mL
40 mM 0.0469 mL 0.2343 mL 0.4687 mL 1.1716 mL
50 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9373 mL
60 mM 0.0312 mL 0.1562 mL 0.3124 mL 0.7811 mL
80 mM 0.0234 mL 0.1172 mL 0.2343 mL 0.5858 mL
100 mM 0.0187 mL 0.0937 mL 0.1875 mL 0.4687 mL
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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.

Keywords:

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

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