SBI-0206965

Catalog No.S7885 Batch:S788501

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Technical Data

Formula

C21H21BrN4O5
Molecular Weight 489.32 CAS No. 1884220-36-3
Solubility (25°C)* In vitro DMSO 97 mg/mL (198.23 mM)
Ethanol 10 mg/mL (20.43 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[2]
  • Cell lines

    A498 cells

  • Concentrations

    10 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of drug for 24 h.
Animal Study:

[2]
  • Animal Models

    Male BALB/c nude mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Customer Product Validation

, , Biochim Biophys Acta, 2017, 1863(11):2796-2807

Selleck's SBI-0206965 has been cited by 37 publications

STING orchestrates the neuronal inflammatory stress response in multiple sclerosis [ Cell, 2024, 187(15):4043-4060.e30] PubMed: 38878778
mTORC1 restricts TFE3 activity by auto-regulating its presence on lysosomes [ Mol Cell, 2024, S1097-2765(24)00832-3] PubMed: 39486419
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] PubMed: 39264808
A multiplexed siRNA screen identifies key kinase signaling networks of brain glia [ Life Sci Alliance, 2023, 6(5)e202201605] PubMed: 36878638
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] PubMed: 35051357
Spatially resolved phosphoproteomics reveals fibroblast growth factor receptor recycling-driven regulation of autophagy and survival [ Nat Commun, 2022, 13(1):6589] PubMed: 36329028
Autophagy Enhances Longevity of Induced Pluripotent Stem Cell-Derived Endothelium via mTOR-Independent ULK1 Kinase [ Stem Cells Transl Med, 2022, 11(11):1151-1164] PubMed: 36173887
TP53 loss-of-function causes vulnerability to autophagy inhibition in aggressive prostate cancer [ Int J Urol, 2022, 29(9):1085-1094] PubMed: 35975690
PKCλ/ι inhibition activates an ULK2-mediated interferon response to repress tumorigenesis [ Mol Cell, 2021, S1097-2765(21)00729-2] PubMed: 34560002
Plasmalogens regulate the AKT-ULK1 signaling pathway to control the position of the axon initial segment [ Prog Neurobiol, 2021, S0301-0082(21)00137-4] PubMed: 34302896

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.