| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H21BrN4O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
SBI-0206965 is a potent, selective, cell-permeable inhibitor of the autophagy kinase ULK1, with IC50 values of 108 nM for ULK1 and 711 nM for the closely related kinase ULK2. It is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation[1][2][3]. It is supplied as a white to off-white solid (C21H21BrN4O5, MW 489.32) at 99.92% purity.
Physical & Chemical Properties
| CAS Number | 1884220-36-3 |
|---|---|
| Molecular Formula | C21H21BrN4O5 |
| Molecular Weight | 489.32 g/mol |
| Purity | 99.92% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CNC(C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br)=O |
| Target | ULK1, ULK2 |
| Signaling Pathway | Autophagy; PI3K/Akt/mTOR; Epigenetics; Apoptosis |
| Solubility | 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. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
ULK1 108 nM (IC50) |
ULK2 711 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (204.37 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.11 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.11 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In A498 and ACHN cells under starvation, SBI-0206965 (5-20 μM; 24 hours) induces apoptosis[1]. SBI-0206965 (5-20 μM; 24 hours) also reduces phosphorylation of Ser108 on the AMPK β1 subunit and raises the levels of cleaved Caspase 8 and PARP, which are markers of apoptosis[1].
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
In A498 xenograft tumors, SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibits tumor growth and induces apoptosis[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Targeting TRPV1-mediated autophagy attenuates nitrogen mustard-induced dermal toxicity. Signal Transduct Target Ther 2021 Jan 25;6(1):29. PMID: 33487631
Stress dynamically modulates neuronal autophagy to gate depression onset. Nature 2025 May;641(8062):427-437. PMID: 40205038
Inhibition of mTOR induces a paused pluripotent state. Nature 2016 Dec 1;540(7631):119-123.
Reduced ULK1 links impaired autophagy and mitophagy to Alzheimer's disease pathology. Nat Aging 2026 May 14. PMID: 42135576
USF2 restricts enterovirus replication and transmission by inhibiting autophagy and vesicle-mediated viral spread. Autophagy 2026 May 22:1-17. PMID: 42152487
TRIM21-mediated ubiquitination of SQSTM1/p62 abolishes its Ser403 phosphorylation and enhances palmitic acid cytotoxicity. Autophagy 2025 Jan;21(1):178-190. PMID: 39172027
PRRSV utilizes MALT1-regulated autophagy flux to switch virus spread and reserve. Autophagy 2024 Dec;20(12):2697-2718. PMID: 39081059
m6A mRNA methylation regulates testosterone synthesis through modulating autophagy in Leydig cells. Autophagy 2021 Feb;17(2):457-475.
Hepatic glycogen directly regulates gluconeogenesis through an AMPK/CRTC2 axis in mice. J Clin Invest 2025 Jun 2;135(11):e188363. PMID: 40454488
PP2Ac Regulates Autophagy via Mediating mTORC1 and ULK1 During Osteoclastogenesis in the Subchondral Bone of Osteoarthritis. Adv Sci (Weinh) 2024 Sep;11(36):e2404080. PMID: 39041921
