SBI-0206965

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SBI-0206965 is a novel inhibitor of the autophagy-initiating kinase ULK1.
    ULK1 (Unc-51 like Autophagy Activating Kinase 1) is a serine/threonine-protein kinase involved in autophagy in starvation. It is an AMPK regulator, a downstream effector and negative regulator of mTORC1. It also plays a role in neuronal differentiation. [1]
    In A549 cells, 5 mM SBI-0206965 strongly suppresses the AZD8055 induced autophagy effect. In SBI-0206965 treated MEFs, after 18 hours of amino acid deprivation, 42% of 6965-treated cells shows 7-AAD and AnnexinV (end stage apoptosis). SBI-02066965 also promotes apoptosis
    in the nutrient-starved state in human U87MG glioblastoma cells and in murine lung carcinoma cells. Moreover, 5 mM SBI-0206965 triggers apoptosis in 23% of cells when combined with AZD8055 versus 10% of cells in the absence of AZD8055 and 7% of cells treated with AZD8055
    alone. Similar to AZD8055, both rapamycin and INK128 exhibits a mild apoptotic response on their own in A549 cells but significantly enhances this apoptotic response when combined with SBI-0206965. [1]
- Properties
  - Alternative Name
    
    (Z)-2-((5-bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzimidic acid
    
    CAS Number
    
    1884220-36-3
    
    Molecular Formula
    
    C21H21BrN4O5
    
    Molecular Weight
    
    489.32
    
    Appearance
    
    A solid
    
    Purity
    
    98.55%
    
    Solubility
    
    ≥24.47 mg/mL in DMSO; insoluble in H2O; ≥5 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mathieu Paquette, Leeanna El-Houjeiri, et al. "AMPK-dependent phosphorylation is required for transcriptional activation of TFEB and TFE3." Autophagy. 2021 Dec;17(12):3957-3975. PMID:33734022
    2. Yoon-Jin Kim, Qingyao Kong, et al. "An autophagy-related protein Becn2 regulates cocaine reward behaviors in the dopaminergic system." Sci Adv. 2021 Feb 19;7(8):eabc8310. PMID:33608268
    3. Vahsen BF, Ribas VT, et al. "Inhibition of the autophagic protein ULK1 attenuates axonal degeneration in vitro and in vivo, enhances translation, and modulates splicing." Cell Death Differ. 2020;10.1038/s41418-020-0543-y. PMID:32341448
    4. Dite TA, Langendorf CG, et al. "AMP-activated protein kinase selectively inhibited by the type II inhibitor SBI-0206965." J Biol Chem. 2018 Jun 8;293(23):8874-8885. PMID:29695504
    5. Dite TA, Ling NXY, et al. "The autophagy initiator ULK1 sensitizes AMPK to allosteric drugs." Nat Commun. 2017 Sep 18;8(1):571. PMID:28924239

SBI-0206965

Background

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