SBI-0206965

製品コードS7885 バッチS788504

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₂₁BrN₄O₅

分子量

489.32

CAS No.

1884220-36-3

Solubility (25°C)*

体外

DMSO

98 mg/mL (200.27 mM)

Ethanol (warmed with 50ºC water bath)

11 mg/mL (22.48 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ	ULK1 kinase assays
キナーゼアッセイ	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.
細胞アッセイ	細胞株	A498 cells
	濃度	10 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of this compound for 24 h.
動物実験	動物モデル	Male BALB/c nude mice
	投薬量	50 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/26118643/
https://pubmed.ncbi.nlm.nih.gov/30078736/

カスタマーフィードバック

: , , Biochim Biophys Acta, 2017, 1863(11):2796-2807

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Oncogenic RAS induces a distinctive form of non-canonical autophagy mediated by the P38-ULK1-PI4KB axis [ Cell Res, 2025, 10.1038/s41422-025-01085-9]	PubMed: 40055523
Inhibiting autophagy selectively prunes dysfunctional tumor vessels and optimizes the tumor immune microenvironment [ Theranostics, 2025, 15(1):258-276]	PubMed: 39744218
STING orchestrates the neuronal inflammatory stress response in multiple sclerosis [ Cell, 2024, 187(15):4043-4060.e30]	PubMed: 38878778
mTORC1 restricts TFE3 activity by auto-regulating its presence on lysosomes [ Mol Cell, 2024, S1097-2765(24)00832-3]	PubMed: 39486419
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728]	PubMed: 39264808
An AMBRA1, ULK1 and PP2A regulatory network regulates cytotoxic T cell differentiation via TFEB activation [ Sci Rep, 2024, 14(1):31838]	PubMed: 39738384
Rigosertib promotes anti-tumor immunity via autophagic degradation of PD-L1 in colorectal cancer cells [ Cancer Lett, 2023, 577:216422]	PubMed: 37805162
A multiplexed siRNA screen identifies key kinase signaling networks of brain glia [ Life Sci Alliance, 2023, 6(5)e202201605]	PubMed: 36878638
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0]	PubMed: 35051357
Spatially resolved phosphoproteomics reveals fibroblast growth factor receptor recycling-driven regulation of autophagy and survival [ Nat Commun, 2022, 13(1):6589]	PubMed: 36329028

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。