Home Autophagy ULK inhibitor - Autophagy inhibitor - Apoptosis related activator SBI-0206965 For research use only.

SBI-0206965

SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.

SBI-0206965 Chemical Structure

SBI-0206965 Chemical Structure

CAS No. 1884220-36-3

Purity & Quality Control

SBI-0206965 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Malme-3M cells Function assay Inhibition of FLAG-tagged ULK1 (unknown origin) expressed in HEK293T cells using GST-labelled Atg101 as substrate in presence of gamma-[32]P-ATP,IC50=0.108 µM. 29211480
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Biological Activity

Description SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Targets
ULK1 [1]
(Cell-free assay)		 ULK2 [1]
(Cell-free assay)
108 nM 711 nM
In vitro
In vitro

In HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death. [1]
Kinase Assay ULK1 kinase assays
γ-32P-ATP assays to measure ULK1 kinase activity are performed. Briefly, Flag-ULK1 is transfected into HEK-293T cells and 20 hours later treated as indicated. The immmunoprecipitate is washed in IP buffer 3 times, and washed in kinase buffer (25 mM MOPS, pH 7.5, 1 mM EGTA, 0.1 mM Na3VO4, 15 mM MgCl2,). Hot and cold ATP are added at a 100 μM final concentration. As substrates, GST or the recombinant protein GST-Atg101 purified from E. coli were used at 1 μg for each reaction. Reactions are boiled and run out on SDS-PAGE gels. Gels are dried and imaged using PhosphoImager software.
Cell Research Cell lines A498 cells
Concentrations 10 μM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AMPK β1 / AMPK β1 / PARP / cleaved PARP / Caspase 8 / cleaved caspase 8 / LC3B I / LC3B II / p62 pACC / ACC / AMPK-pThr-172 30078736

Chemical Information & Solubility

Molecular Weight 489.32 Formula

C21H21BrN4O5
CAS No. 1884220-36-3 SDF Download SBI-0206965 SDF
Smiles CNC(=O)C1=CC=CC=C1OC2=NC(=NC=C2Br)NC3=CC(=C(C(=C3)OC)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 98 mg/mL ( (200.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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