BL-918

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BL-918 是 ULK1 的小分子激活剂，EC50 为 24 nM（100 nM 时激酶活性为 243%）。

BL-918 is a small molecule activator of ULK1 with EC50 of 24 nM (243% kinase activity at 100 nM), induces autophagy via the ULK complex in SH-SY5Y cells; displays a cytoprotective effect on MPP+-treated SH-SY5Y cells, as well as protected against MPTP-induced motor dysfunction and loss of dopaminergic neurons by targeting ULK1-modulated autophagy in mouse models of PD.

Cell Autophagy Assay Cell Line:SH-SY5Y cells Concentration:5 μM Incubation Time:For 24 hoursResult:Induced Autophagy.Cell Viability Assay 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 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.

Animal Model:Male C57BL/6 mice (eight-week old) weighing between 20 and 25 gDosage: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.

BL918

Autophagy

ULK

ULK

——

——

2101517-69-3

533.44

C23H15F8N3OS

>98% (HPLC)

In Vitro:?DMSO : ≥ 250 mg/mL (468.66 mM)

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

(R)-2-(3-(3,5-Bis(trifluoromethyl)phenyl)thioureido)-N-(2,4-difluorophenyl)-2-phenylacetamide

(-20℃)

With Ice Pack

≥ 2 years