BL-918 是一种具有口服活性 UNC-51 样激酶 1 (ULK1) 激活剂，EC₅₀ 为 24.14 nM。BL-918 通过靶向 ULK 复合物发挥其细胞保护性自噬作用。BL-918 有用于帕金森氏病 (PD) 的潜力。

BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC 50 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.

Solid

ULK1 24.14 nM (EC50) ULK1 0.719 μM (Kd)

BL-918 (compound 33i) binds to ULK1 with a high binding affinity (KD=0.719 μM).
BL-918 (5 μM; for 24 hours) induces autophagy in Neuron-Like SH-SY5Y cells.
BL-918 (0.5-50 μM; for 24 hours) can partially reverse MPP-induced cell death, which is determined by enhancing cell viability.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

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

In Vitro: DMSO : ≥ 250 mg/mL (468.66 mM)配制储备液