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SBI-0206965 ULK inhibitor

Cat.No.S7885

SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. This compound inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.

Chemical Structure

Molecular Weight: 489.32

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Autophagy CXCR Nrf2 Mitophagy LRRK2 FKBP Heme Oxygenase LC3 cGAS OGA Beclin
Related Products	MRT68921 HCl ULK-101 LYN-1604 XST-14 BL-918 SBP-7455 Phospho-ULK1 (Ser555) Antibody [N1G15] DCC-3116 ULK1 Antibody [A14P9] Phospho-ULK1 (Ser757) Antibody [A12P8] ULK1 Antibody [K18A5]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
human Malme-3M cells	Function assay	Inhibition of FLAG-tagged ULK1 (unknown origin) expressed in HEK293T cells using GST-labelled Atg101 as substrate in presence of gamma-[32]P-ATP,IC50=0.108 µM.	29211480



Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	489.32	Formula	C₂₁H₂₁BrN₄O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1884220-36-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CNC(=O)C1=CC=CC=C1OC2=NC(=NC=C2Br)NC3=CC(=C(C(=C3)OC)OC)OC

Solubility

In vitro
Batch:

DMSO : 98 mg/mL (200.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (5.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	ULK1 ^[1] (Cell-free assay) 108 nM ULK2 ^[1] (Cell-free assay) 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. This compound suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, it also synergizes with mTOR inhibition to induce cancer cell death. ^[1]
Kinase Assay	ULK1 kinase assays
Kinase Assay	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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26118643/ [2] https://pubmed.ncbi.nlm.nih.gov/30078736/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-AMPK β1 / AMPK β1 / PARP / cleaved PARP / Caspase 8 / cleaved caspase 8 / LC3B I / LC3B II / p62 pACC / ACC / AMPK-pThr-172		30078736

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