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My CartCAS：676596-65-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 676596-65-9 |
| Name | 1-Azakenpaullone |
| Molecular Formula | C15 H10 Br N3 O |
| Molecular Weight | 328.16 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-258-5 |
| MDL | MFCD09037522 |
| SMILES | O=C(NC1=CC=CN=C12)CC3=C2NC4=C3C=C(Br)C=C4 |
| Target Point | GSK-3 |
| Passage | PI3K/Akt/mTOR;Stem Cells |
| Background | 1-Azakenpaullone is a highly selective GSK-3β inhibitor. |
| Biological Activity | 1-Azakenpaullone可选择性抑制CDK1/cyclin B、CDK5/p25和GSK-3β活性, IC50值分别为0.018 μM、 4.2 μM和2.0 μM。[1] |
| In Vitro | 在人胰岛细胞中，1-Azakenpaullone(5 mM)和葡萄糖(8 mM)联合可抑制β细胞的增殖。[2] 1-Azakenpaullone可有效诱导INS-1E细胞复制，并保护INS-1E细胞免于脂糖毒性引起的细胞死亡。[3][4] |
| In Vivo | 1-Azakenpaullone(10 或100 pmol，脑内注射)预处理可减弱克他命引起的运动亢进、PPI中断、认知缺陷，并在转动试验中提高克他命引起的运动不协调。 |
| Cell Experiment | Animal Models: 雄性 NMRI小鼠;Dosages: ~500 pmol;Administration: 脑内注射[5] |
| Animal Experiment | Cell lines: INS-1E β细胞系;Concentrations: 20 μM;Incubation Time: 4 天[4] |
| Kinase Experiment | 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.)[6] |
| Data Literature Source | [1] Kunick C，et al. Bioorg Med Chem Lett. 2004，14(2)，413-416. [2] Liu H，et al. Diabetes. 2009，58(3)，663-672. [3] Stukenbrock H，et al. J Med Chem. 2008，51(7)，2196-2207. [4] Mussmann R，et al. J Biol Chem. 2007，282(16)，12030-12037. [5] Chan MH，et al. Schizophr Res. 2012，136(1-3)，96-103. [6] Leost M，et al. Eur J Biochem. 2000，267(19)，5983-5994. |
| Unit | Bottle |
| Specification | 2mg |
是一种高度选择性GSK-3β抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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