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BL-918

CAS No. : 2101517-69-3

MCE 国际站：BL-918

产品活性：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。

研究领域：Autophagy

作用靶点：ULK | Autophagy

In Vitro: BL-918 (compound 33i) binds to ULK1 with a high binding affinity (K_D=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.

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).

相关产品：Bioactive Compound Library Plus | Kinase Inhibitor Library | Autophagy Compound Library | Anti-Aging Compound Library | Orally Active Compound Library | MRT67307 | MRT68921 dihydrochloride | ULK-101 | GW406108X

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