SBI-0206965
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.92%
- No. CAS: 1884220-36-3
- Fòrmula: C21H21BrN4O5
- Peso molecular:489.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) SBI-0206965
More- Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]
- Nature. 2025 May;641(8062):427-437. [Abstract]
- Nature. 2016 Dec 1;540(7631):119-123. [Abstract]
- Autophagy. 2025 Jan;21(1):178-190. [Abstract]
- Autophagy. 2024 Dec;20(12):2697-2718. [Abstract]
- Autophagy. 2021 Feb;17(2):457-475. [Abstract]
- Adv Sci (Weinh). 2024 Jul 23:e2404080. [Abstract]
- J Clin Invest. 2025 Jun 2;135(11):e188363. [Abstract]
- EBioMedicine. 2018 Aug:34:85-93. [Abstract]
- Int J Biol Sci. 2021 Jul 5;17(11):2772-2794. [Abstract]
- Free Radic Biol Med. 2024 Nov 1:224:846-861. [Abstract]
- Stem Cell Res Ther. 2025 Apr 24;16(1):206. [Abstract]
- Cell Rep. 2021 Jul 20;36(3):109398. [Abstract]
- Antioxidants (Basel). 2025 Mar 7;14(3):322. [Abstract]
- Cell Biol Toxicol. 2025 Jan 28;41(1):35. [Abstract]
- Mol Cancer Ther. 2020 Feb;19(2):590-601. [Abstract]
- PLoS Pathog. 2025 Jul 16;21(7):e1013319. [Abstract]
- Int Immunopharmacol. 2022 Jul:108:108869. [Abstract]
- Biochem J. 2025 Jul 22:BCJ20240731. [Abstract]
- FASEB J. 2024 May 31;38(10):e23671. [Abstract]
- iScience. 2023 Apr 7;26(5):106598. [Abstract]
- Sci Rep. 2025 Oct 14;15(1):35808. [Abstract]
- J Virol. 2024 Dec 6:e0144924. [Abstract]
- Cell Signal. 2024 Jun:118:111136. [Abstract]
- Mol Med Rep. 2026 Apr;33(4):116. [Abstract]
- Vet Res. 2025 Apr 23;56(1):87. [Abstract]
- Food Chem Toxicol. 2021 Feb:148:111957. [Abstract]
- Cosmetics. 2024 Mar 1, 11(2), 35.
- Anim Cells Syst. 2023 Nov 27.
- Mol Biol Rep. 2025 Oct 9;52(1):1000. [Abstract]
- Int J Biochem Cell Biol. 2022 May;146:106208. [Abstract]
- Oncologie. 2024 Feb 23.
- bioRxiv. 2026 Apr 17:2026.04.15.717889. [Abstract]
- 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. 2021 Nov 15:2021:2896674. [Abstract]
- Taiwan Veterinary Journal. 2021, Jun.
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Ver todos los productos específicos de isoformas AMPK
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Actividad biológica
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ULK1 108 nM (IC50) |
ULK2 711 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
6.78 μM
Compound: SBI-0206963; SBI-0206965
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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
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[PMID: 32961380] |
| HL-60 | IC50 |
18.92 μM
Compound: SBI-0206963; SBI-0206965
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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
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[PMID: 32961380] |
| MCF7 | IC50 |
26.17 μM
Compound: SBI-0206963; SBI-0206965
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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
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[PMID: 32961380] |
| MDA-MB-468 | IC50 |
18.38 μM
Compound: SBI-0206963; SBI-0206965
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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
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[PMID: 32961380] |
| MDA-MB-468 | IC50 |
2.1 μM
Compound: 1; SBI-0206965
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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
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[PMID: 33200929] |
| U-937 | IC50 |
25.12 μM
Compound: SBI-0206963; SBI-0206965
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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
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[PMID: 32961380] |
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.
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Cell Line:A498 and ACHN cells (starvation medium (EBSS) treatment)
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Concentration:5, 10 ,20 μM
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Incubation Time:24 hours
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Result:Induced significant levels of apoptosis.
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Cell Line:A498 and ACHN cells (EBSS treatment)
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Concentration:5, 10, 20 μM
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Incubation Time:24 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male BALB/c nude mice (A498 xenograft tumours)[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; once every three days for 37 days
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Result:Significantly suppressed tumour growth.
Chemical Information
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No. CAS 1884220-36-3
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Appearance Solid
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Peso molecular 489.32
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Fòrmula C21H21BrN4O5
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Color White to off-white
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SMILES
CNC(C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (41)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
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.
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Nature
2025 May;641(8062):427-437. PMID: 40205038 -
Nature
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
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.
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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.
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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
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.
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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
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
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 -
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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 -
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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 -
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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 -
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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