1-Azakenpaullone

製品コードS7193 バッチS719301

印刷

化学情報

Synonyms

1-Akp

Storage
(From the date of receipt)

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

化学式

C₁₅ H₁₀ Br N₃ O

分子量

328.16

CAS No.

676596-65-9

Solubility (25°C)*

体外

DMSO

66 mg/mL (201.12 mM)

Water

Insoluble

Ethanol

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 40%PEG300 2 5%Tween80 3 50%ddH2O 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。	3.300mg/ml (10.06mM)	Taking the 1 mL working solution as an example, add 50 μL 66 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. 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	1-Azakenpaullone (1-Akp)は、GSK-3βの強力かつ選択的阻害剤であり、IC50は18 nM、CDK1/cyclin BおよびCDK5/p25に対して100倍以上の選択性を示します。
in vitro	1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. In human islets, this compound (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. It effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death.
in vivo	Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the induced locomotor hyperactivity, disruption of PPI and cognitive deﬁcits, and improves the induced motor incoordination in rotarod test.

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase preparations and assays
キナーゼアッセイ	GSK-3β is assayed, following a 1/100 dilution in 1 mg BSA per mL 10 mM dithiothreitol, with 5 μL 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM [γ-³²P]ATP (3000 Ci·mmol^-1; 1 mCi·mL^-1 ) in a final volume of 30 μL. After 30 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto 2.5×3 cm pieces of Whatman P81 phosphocellulose paper, and 20 s later, the filters are washed five times in a solution of 10 mL phosphoric acid per L of water. The wet filters are counted in the presence of 1 mL ACS scintillation fluid. The kinase activity of CDK1/cyclin B is assayed in buffer C, with 1 mg/mL histone H1, in the presence of 15 μM [γ-32P]ATP (3000 Ci·mmol^-1; 1 mCi·mL^-1 ) in a final volume of 30 μL. After 10 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto P81 phosphocellulose papers and treated as described above. The activity of CDK5/p25 is assayed in buffer C as described for CDK1/cyclin B. (Buffer A: 10 mM MgCl2 , 1 mM EGTA, 1 mM dithiothreitol, 25 mM Tris/HCl pH 7.5. Buffer C: homogenization buffer but 5 mM EGTA, no NaF and no protease inhibitors.)
細胞アッセイ	細胞株	INS-1E β cell
	濃度	20 μM
	反応時間	4 days
	実験の流れ	Cell replication is determined by BrdUrd incorporation after treatment with 1-Azakenpaullone for 24 h. The relative cell number is determined after treatment with this compound for 4 days using the CyQuant cell proliferation assay. Results are presented as fold change relative to control.
動物実験	動物モデル	Male NMRI mice
	投薬量	~500 pmol
	投与方法	i.c.v.

参考

https://pubmed.ncbi.nlm.nih.gov/14698171/
https://pubmed.ncbi.nlm.nih.gov/19073772/
https://pubmed.ncbi.nlm.nih.gov/18345612/

https://pubmed.ncbi.nlm.nih.gov/17242403/
https://pubmed.ncbi.nlm.nih.gov/22325078/
https://pubmed.ncbi.nlm.nih.gov/10998059/

+ 展开

カスタマーフィードバック

: , , Mol Neurobiol, 2018, 55(2):1639-1651

: , , Dev Genes Evol, 2015, 225(1):47-53.

: Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(1):232-242]

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：

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Filamin C regulates skeletal muscle atrophy by stabilizing dishevelled-2 to inhibit autophagy and mitophagy [ Mol Ther Nucleic Acids, 2022, 27:147-164]	PubMed: 34976434
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Modulation of Neuroinflammatory Signaling Enhances the Neurogenic Reprogramming Capacity of Müller Glia Across Species [ The Ohio State University, 2021, ]	PubMed: None
Overexpression of ubiquitin-conjugating enzyme E2 L3 in hepatocellular carcinoma potentiates apoptosis evasion by inhibiting the GSK3β/p65 pathway. [ Cancer Lett, 2020, 1;481:1-14]	PubMed: 32268166
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BYSL Promotes Glioblastoma Cell Migration, Invasion, and Mesenchymal Transition Through the GSK-3β/β-Catenin Signaling Pathway [ Front Oncol, 2020, 10:565225]	PubMed: 33178594

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。