S80497 |
SBI-0206965 |
| 源叶(MedMol) | 98% |
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- 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)
- 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
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