SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2.
体外研究
SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation.
SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis.
Apoptosis Analysis
Cell Line:
A498 and ACHN cells (starvation medium (EBSS) treatment)
Concentration:
5, 10 ,20 μM
Incubation Time:
24 hours
Result:
Induced significant levels of apoptosis.
Western Blot Analysis
Cell Line:
A498 and ACHN cells (EBSS treatment)
Concentration:
5, 10, 20 μM
Incubation Time:
24 hours
Result:
Attenuated the phosphorylation of Ser108 of the AMPK β1 subunit and increased the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluated by analysis of LC3B and p62.
体内研究
SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours.
Animal Model:
Six-week-old male BALB/c nude mice (A498 xenograft tumours)
Dosage:
50 mg/kg
Administration:
Intraperitoneal injection; once every three days for 37 days
Result:
Significantly suppressed tumour growth.
分子式
C21H21BrN4O5
分子量
489.32
CAS号
1884220-36-3
运输条件
Room temperature in continental US; may vary elsewhere.