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SBI-0206965 ULK1 inhibitor

Catalog No.A8715
Size Price Stock 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]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. 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
2. 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

Quality Control

Chemical structure

SBI-0206965

Related Biological Data

SBI-0206965

Related Biological Data

SBI-0206965

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 > 24.5mg/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.

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Chemical Properties

Cas No. 1884220-36-3 SDF Download SDF
Synonyms N/A
Chemical Name (Z)-2-((5-bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzimidic acid
Canonical SMILES C/N=C(O)/C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br
Formula C21H21BrN4O5 M.Wt 489.32
Solubility >24.5mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.