1-Azakenpaullone

製品コードS7193 バッチS719301

印刷

化学情報

Chemical Structure 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）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.3mg/ml 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) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.
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. [1] In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. [2] 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death. [3][4]
in vivo Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the ketamine-induced locomotor hyperactivity, disruption of PPI and cognitive deficits, and improves the ketamine-induced motor incoordination in rotarod test. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase preparations and assays
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, 50 μg heparin/mL. 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 1-Azakenpaullone 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.

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：

Patterns of NFkB activation resulting from damage, reactive microglia, cytokines, and growth factors in the mouse retina [ Exp Neurol, 2023, 359:114233] PubMed: 36174748
Induction of mouse totipotent stem cells by a defined chemical cocktail [ Nature, 2022, 10.1038/s41586-022-04967-9] PubMed: 35728625
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
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
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
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] PubMed: 31740922
BYSL Promotes Glioblastoma Cell Migration, Invasion, and Mesenchymal Transition Through the GSK-3β/β-Catenin Signaling Pathway [ Front Oncol, 2020, 10:565225] PubMed: 33178594
Targeting Degradation of the Transcription Factor C/EBPβ Reduces Lung Fibrosis by Restoring Activity of the Ubiquitin-Editing Enzyme A20 in Macrophages [ Immunity, 2019, 51(3-:522-534] PubMed: 31471107
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] PubMed: 31160710
Acquired Resistance to FGFR Inhibitor in Diffuse-Type Gastric Cancer through an AKT-Independent PKC-Mediated Phosphorylation of GSK3β [Lau WM, et al. Mol Cancer Ther, 2018, 17(1):232-242] PubMed: 28978722

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。

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