SBI-0206965 - ULK1 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESBI-0206965Cat. No.: HY-16966CAS No.: 1884220-36-3分式: CHBrNO分量: 489.32作靶点: ULK; Autophagy; Apoptosis作通路: Autophagy; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (204.3

2、7 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.11 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.11 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 SBI-0206965种强效, 选择性和细胞渗透性噬激酶 ULK1 抑制剂, 抑制 ULK1 和 ULK2 激

3、酶活性, IC50 值分别为 108 nM 和 711 nM。IC50 & Target IC50: 108 nM (ULK1 kinase), 711 nM (ULK2 kinase) 2体外研究 SBI-0206965 (5-20 M; 24 hours) induces apoptosis of A498 and ACHN cells during starvation 1.SBI-0206965 (5-20 M; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK 1 subunit andincreases t

4、he levels of cleaved Caspase 8 and PARP, markers of apoptosis 1.Apoptosis Analysis 1Cell Line: A498 and ACHN cells (starvation medium (EBSS) treatment)Concentration: 5, 10 ,20 MIncubation Time: 24 hoursResult: Induced significant levels of apoptosis.Western Blot Analysis 1Cell Line: A498 and ACHN ce

5、lls (EBSS treatment)Concentration: 5, 10, 20MIncubation Time: 24 hoursResult: Attenuated the phosphorylation of Ser108 of the AMPK 1 subunit and increased thelevels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluatedby analysis of LC3B and p62.体内研究 SBI-0206965 (50mg/kg; i.p.

6、; once every 3 days for 37 days) inhibites tumour growth and induces apoptosisin A498 xenograft tumours 1.Animal Model: Six-week-old male BALB/c nude mice (A498 xenograft tumours) 1Dosage: 50mg/kgAdministration: Intraperitoneal injection; once every three days for 37 daysResult: Significantly suppre

7、ssed tumour growth.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Nature. 2016 Dec 1;540(7631):119-123. BioMedicine. 2018 Aug;34:85-93.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for

8、Clear Cell RenalCarcinoma and the Antitumor Effectsof 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 Jul16;59(2):285-97.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo