| 产品描述： | 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 |
| 靶点： |
ULK1:108 nM (IC50);ULK2:711 nM (IC50);Apoptosis;Autophagy |
| 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. |
| 参考文献： |
1. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell RenalCarcinoma and the Antitumor Effects of SBI-0206965. EBioMedicine. 2018 Aug;34:85-93. 2. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-97. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.044 ml |
10.218 ml |
20.437 ml |
| 5 mM |
0.409 ml |
2.044 ml |
4.087 ml |
| 10 mM |
0.204 ml |
1.022 ml |
2.044 ml |
| 50 mM |
0.041 ml |
0.204 ml |
0.409 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京