Toggle Nav
Close
  • Menu
  • Setting

SBI-0206965

Catalog No.
A8715
ULK1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
5mg
$100.00
In stock
25mg
$350.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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]

Reference:
[1] Egan DF, Chun MG, Vamos M et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16; 59 (2): 285-97.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt489.32
Cas No.1884220-36-3
FormulaC21H21BrN4O5
Solubility≥24.5 mg/mL in DMSO
Chemical Name(Z)-2-((5-bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzimidic acid
SDFDownload SDF
Canonical SMILESC/N=C(O)/C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

HEK293T cells transfected with WT or KI Myc-tagged ULK1 and WT Vps34

Preparation method

The solubility of this compound in DMSO is >24.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Reacting condition

1, 10 and 50 μM; 1 hr

Applications

In HEK293T cells transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibited Ser249 phosphorylation of overexpressed Vps34 at the dose of ~5 μM. In HEK293T cells, it was found that SBI-0206965 also inhibited the phosphorylation of Beclin1 Ser15 to comparable extents.

References:

[1] Egan DF, Chun MG, Vamos M et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16; 59 (2): 285-97.

Quality Control

Chemical structure

SBI-0206965

Related Biological Data

SBI-0206965

Related Biological Data

SBI-0206965