BL-918_product_DataBase

Bioactivity

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].

Invitro

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]. Cell Autophagy Assay[1] Cell Line:

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]. Animal Model:

Name

BL-918

CAS

2101517-69-3

Formula

C23H15F8N3OS

Molar Mass

533.44

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Ouyang L, et al. Small-Molecule Activator of UNC-51-Like Kinase 1 (ULK1) That Induces Cytoprotective Autophagy for Parkinson's Disease Treatment. J Med Chem. 2018 Apr 12;61(7):2776-2792.

PeptideDB

BL-918

CAS: 2101517-69-3 F: C23H15F8N3OS W: 533.44