SBI-0206965

Catalog No.S7885

SBI-0206965 Chemical Structure

Molecular Weight(MW): 489.32

SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.

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1 Customer Review

  • Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, ** p < 0.01, *** p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05.

    Biochim Biophys Acta, 2017, 1863(11):2796-2807. SBI-0206965 purchased from Selleck.

Purity & Quality Control

Choose Selective Autophagy Inhibitors

Biological Activity

Description SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.
Targets
ULK1 [1]
(Cell-free assay)
ULK2 [1]
(Cell-free assay)
108 nM 711 nM
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]

Protocol

Solubility (25°C)

In vitro DMSO 97 mg/mL (198.23 mM)
Ethanol 10 mg/mL warmed (20.43 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 489.32
Formula

C21H21BrN4O5

CAS No. 1884220-36-3
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID