Art. -Nr.: HY-16966

SBI-0206965

41 Cited Publications

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Based on 41 publication(s) in Google Scholar

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2. SBI-0206965 is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation.

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Reinheit: 99.92%
CAS. Nr.: 1884220-36-3
Formel: C₂₁H₂₁BrN₄O₅
Molecular Weight:489.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SBI-0206965 Chemical Structure

CAS. Nr.: 1884220-36-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (41)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ULK1

108 nM (IC₅₀)

ULK2

711 nM (IC₅₀)

Alle ULK Isoform-spezifische Produkte anzeigen :

ULK1
ULK2

Alle AMPK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	6.78 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
HL-60	IC₅₀	18.92 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MCF7	IC₅₀	26.17 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MDA-MB-468	IC₅₀	18.38 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MDA-MB-468	IC₅₀	2.1 μM Compound: 1; SBI-0206965	Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 33200929]
U-937	IC₅₀	25.12 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]

In Vitro

SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation^[1].
SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

A498 and ACHN cells (starvation medium (EBSS) treatment)
Concentration:

5, 10 ,20 μM
Incubation Time:

24 hours
Result:

Induced significant levels of apoptosis.

Western Blot Analysis^[1]

Cell Line:

A498 and ACHN cells (EBSS treatment)
Concentration:

5, 10, 20 μM
Incubation Time:

24 hours
Result:

Attenuated the phosphorylation of Ser108 of the AMPK β1 subunit and increased the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluated by analysis of LC3B and p62.

In Vivo

SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Six-week-old male BALB/c nude mice (A498 xenograft tumours)^[1]
Dosage:

50 mg/kg
Administration:

Intraperitoneal injection; once every three days for 37 days
Result:

Significantly suppressed tumour growth.

Chemical Information

CAS. Nr. 1884220-36-3
Appearance Solid
Molecular Weight 489.32
Formel C₂₁H₂₁BrN₄O₅
Color White to off-white
SMILES

CNC(C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (41)

All WB2D/3D Cell Culture and Differentiation

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Journal Impact Factor

Signal Transduct Target Ther

Targeting TRPV1-mediated autophagy attenuates nitrogen mustard-induced dermal toxicity. [Abstract]

2021 Jan 25;6(1):29. PMID: 33487631

SBI-0206965 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]

SBI-0206965 (SBI, 10 μM, 25 h) prevented Nitrogen mustard-induced autophagy in keratinocytes.

SBI-0206965 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]

SBI-0206965 (SBI, 10 μM, 25 h) restored cell viability following Nitrogen mustard treatment of keratinocytes.
Nature

Stress dynamically modulates neuronal autophagy to gate depression onset. [Abstract]

2025 May;641(8062):427-437. PMID: 40205038
Nature

Inhibition of mTOR induces a paused pluripotent state. [Abstract]

2016 Dec 1;540(7631):119-123. PMID: 27880763
Autophagy

TRIM21-mediated ubiquitination of SQSTM1/p62 abolishes its Ser403 phosphorylation and enhances palmitic acid cytotoxicity. [Abstract]

2025 Jan;21(1):178-190. PMID: 39172027
Autophagy

PRRSV utilizes MALT1-regulated autophagy flux to switch virus spread and reserve. [Abstract]

2024 Dec;20(12):2697-2718. PMID: 39081059

SBI-0206965 purchased from MedChemExpress. Usage Cited in: Autophagy. 2024 Dec;20(12):2697-2718. [Abstract]

SBI-0206965 (SBI, 1 μM, 24 h) alleviated the Mi-2-induced LC3-II increase in Marc-145 cells.
Autophagy

m6A mRNA methylation regulates testosterone synthesis through modulating autophagy in Leydig cells. [Abstract]

2021 Feb;17(2):457-475. PMID: 31983283

SBI-0206965 purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Feb;17(2):457-475. [Abstract]

SBI-0206965 (SBI, 2 μM, 7 h) attenuated human chorionic gonadotropin-induced increase of LC3B-II and Ser555 phosphorylation of ULK1, and decrease of SQSTM1 in Leydig cells.
Adv Sci (Weinh)

PP2Ac Regulates Autophagy via Mediating mTORC1 and ULK1 During Osteoclastogenesis in the Subchondral Bone of Osteoarthritis. [Abstract]

2024 Jul 23:e2404080. PMID: 39041921
J Clin Invest

Hepatic glycogen directly regulates gluconeogenesis through an AMPK/CRTC2 axis in mice. [Abstract]

2025 Jun 2;135(11):e188363. PMID: 40454488
EBioMedicine

Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell Renal Carcinoma and the Antitumor Effects of SBI-0206965. [Abstract]

2018 Aug:34:85-93. PMID: 30078736

SBI-0206965 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2018 Aug:34:85-93. [Abstract]

A498 and ACHN cells are cultured in starvation medium (EBSS) with SBI-0206965 (0 μM, 5 μM, 10 μM, and 20 μM) for 24 h. Phosphorylation of Ser108 of the AMPK β1 subunit, cleavage of PARP and Caspase 8, and levels of LC3B and p62 are measured by western blot analysis.
Int J Biol Sci

Crosstalk between hypoxia-sensing ULK1/2 and YAP-driven glycolysis fuels pancreatic ductal adenocarcinoma development. [Abstract]

2021 Jul 5;17(11):2772-2794. PMID: 34345207
Free Radic Biol Med

BL-918 alleviates oxidative stress in rats after subarachnoid hemorrhage by promoting mitophagy through the ULK1/PINK1/Parkin pathway. [Abstract]

2024 Nov 1:224:846-861. PMID: 39368518
Stem Cell Res Ther

Nano-zinc oxide (nZnO) targets the AMPK-ULK1 pathway to promote bone regeneration. [Abstract]

2025 Apr 24;16(1):206. PMID: 40275329
Cell Rep

Neuronal activity recruits the CRTC1/CREB axis to drive transcription-dependent autophagy for maintaining late-phase LTD. [Abstract]

2021 Jul 20;36(3):109398. PMID: 34289350
Antioxidants (Basel)

Procyanidin A1 from Peanut Skin Exerts Anti-Aging Effects and Attenuates Senescence via Antioxidative Stress and Autophagy Induction. [Abstract]

2025 Mar 7;14(3):322. PMID: 40227314
Cell Biol Toxicol

Targeting p38γ synergistically enhances sorafenib-induced cytotoxicity in hepatocellular carcinoma. [Abstract]

2025 Jan 28;41(1):35. PMID: 39871031
Mol Cancer Ther

Dual mTORC1/2 Inhibition Sensitizes Testicular Cancer Models to Cisplatin Treatment. [Abstract]

2020 Feb;19(2):590-601. PMID: 31744897
PLoS Pathog

The African swine fever virus p22 inhibits the JAK-STAT signaling pathway by promoting the TAX1BP1-mediated degradation of the type I interferon receptor. [Abstract]

2025 Jul 16;21(7):e1013319. PMID: 40668839
Int Immunopharmacol

Activation of the AMPK-ULK1 pathway mediated protective autophagy by sevoflurane anesthesia restrains LPS-induced acute lung injury (ALI). [Abstract]

2022 Jul:108:108869. PMID: 35605434
Biochem J

Comparison of Classical P81 and SVI-P Cation-Exchange Papers in Radiometric Protein Kinase Assays. [Abstract]

2025 Jul 22:BCJ20240731. PMID: 40700005
FASEB J

Inhibition of NLRP3 inflammasome by MCC950 under hypoxia alleviates photoreceptor apoptosis via inducing autophagy in Müller glia. [Abstract]

2024 May 31;38(10):e23671. PMID: 38752538
iScience

Amphibian pore-forming protein βγ-CAT drives extracellular nutrient scavenging under cell nutrient deficiency. [Abstract]

2023 Apr 7;26(5):106598. PMID: 37128610
Sci Rep

Pregnane X receptor (PXR) as a prognostic marker and therapeutic target in kidney renal clear cell carcinoma (KIRC) via AMPK pathway regulation. [Abstract]

2025 Oct 14;15(1):35808. PMID: 41087473
J Virol

Potassium molybdate blocks APN-dependent coronavirus entry by degrading receptor via PIK3C3-mediated autophagy. [Abstract]

2024 Dec 6:e0144924. PMID: 39641621
Cell Signal

microRNA-125b-1-3p mediates autophagy via the RRAGD/mTOR/ULK1 signaling pathway and mitigates atherosclerosis progression. [Abstract]

2024 Jun:118:111136. PMID: 38471617
Mol Med Rep

ULK1 activates NCOA4‑mediated ferritinophagy via the Beclin1/VPS34 complex in cardiomyocyte hypertrophy. [Abstract]

2026 Apr;33(4):116. PMID: 41685593
Vet Res

The African swine fever virus B125R protein antagonizes JAK-STAT signalling by promoting the degradation of IFNAR2. [Abstract]

2025 Apr 23;56(1):87. PMID: 40270033
Food Chem Toxicol

Plumbagin induces Ishikawa cell cycle arrest, autophagy, and apoptosis via the PI3K/Akt signaling pathway in endometrial cancer. [Abstract]

2021 Feb:148:111957. PMID: 33383144
Cosmetics

2024 Mar 1, 11(2), 35.
Anim Cells Syst

2023 Nov 27.
Mol Biol Rep

Naringin mitigates liver damage in a tissue-engineered liver of metabolic dysfunction-associated steatotic liver disease model by promoting autophagy via the mTOR-ULK1 pathway. [Abstract]

2025 Oct 9;52(1):1000. PMID: 41066001
Int J Biochem Cell Biol

Trehalose induces B cell autophagy to alleviate myocardial injury via the AMPK/ULK1 signalling pathway in acute viral myocarditis induced by Coxsackie virus B3. [Abstract]

2022 May;146:106208. PMID: 35381374
Oncologie

2024 Feb 23.
bioRxiv

Disturbed ATP and AMPK homeostasis in an Ank F377del mouse model for craniometaphyseal dysplasia. [Abstract]

2026 Apr 17:2026.04.15.717889. PMID: 42039557
SSRN

2025 Jul 25.
University of Pittsburgh

2025.
University of Liege

2024.
bioRxiv

2023 Sep 16.
SSRN

2023 Aug 14.
Research Square Preprint

2023 May 22.
Oxid Med Cell Longev

ULK1 Suppresses Osteoclast Differentiation and Bone Resorption via Inhibiting Syk-JNK through DOK3. [Abstract]

2021 Nov 15:2021:2896674. PMID: 34820053
Taiwan Veterinary Journal

2021, Jun.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (204.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0437 mL

10.2183 mL

20.4365 mL

5 mM

0.4087 mL

2.0437 mL

4.0873 mL

10 mM

0.2044 mL

1.0218 mL

2.0437 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell RenalCarcinoma and the Antitumor Effects of SBI-0206965. EBioMedicine. 2018 Aug;34:85-93. [Content Brief]

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

[3]. Hawley SA, et al. BAY-3827 and SBI-0206965: Potent AMPK Inhibitors That Paradoxically Increase Thr172 Phosphorylation. Int J Mol Sci. 2023 Dec 29;25(1):453. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0437 mL	10.2183 mL	20.4365 mL	51.0913 mL
	5 mM	0.4087 mL	2.0437 mL	4.0873 mL	10.2183 mL
	10 mM	0.2044 mL	1.0218 mL	2.0437 mL	5.1091 mL
	15 mM	0.1362 mL	0.6812 mL	1.3624 mL	3.4061 mL
	20 mM	0.1022 mL	0.5109 mL	1.0218 mL	2.5546 mL
	25 mM	0.0817 mL	0.4087 mL	0.8175 mL	2.0437 mL
	30 mM	0.0681 mL	0.3406 mL	0.6812 mL	1.7030 mL
	40 mM	0.0511 mL	0.2555 mL	0.5109 mL	1.2773 mL
	50 mM	0.0409 mL	0.2044 mL	0.4087 mL	1.0218 mL
	60 mM	0.0341 mL	0.1703 mL	0.3406 mL	0.8515 mL
	80 mM	0.0255 mL	0.1277 mL	0.2555 mL	0.6386 mL
	100 mM	0.0204 mL	0.1022 mL	0.2044 mL	0.5109 mL

Keywords

SBI-0206965

41 Cited Publications

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SBI-0206965

Apoptosis Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SBI-0206965

Alle ULK Isoform-spezifische Produkte anzeigen

Alle AMPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (41)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SBI-0206965 Related Classifications

Art. -Nr.: HY-16966