标签归档：帕罗

肯帕罗酮

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肯帕罗酮

货号：
IK0500

品牌：
Jinpan

肯帕罗酮

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产品简介
MDL MFCD02683595
InChIKey QQUXFYAWXPMDOE-UHFFFAOYSA-N
InChI InChI=1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
PubChem CID 3820
别名 NSC-664704; 9-Bromopaullone
英文名称 Kenpaullone
CAS 142273-20-9
分子式 C16H11BrN2O
分子量 327.18
储存条件 -20度
纯度 ≥98%
单位 瓶
SMILES O=C1NC2=CC=CC=C2C(NC3=C4C=C(Br)C=C3)=C4C1
靶点 CDK;GSK-3β
规格 5mg 10mM*1mL in DMSO 10mg
Kenpaullone是CDKs的ATP竞争性抑制剂， 它同样也抑制GSK3β。

1-氮杂坎帕罗酮

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1-氮杂坎帕罗酮

货号：
IA2800

品牌：
Jinpan

1-氮杂坎帕罗酮

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产品简介
MDL MFCD09037522
描述 是具有高度选择性的、ATP 竞争性的糖原合成酶激酶3 β (GSK-3β) 的抑制剂。
EC EINECS 200-258-5
别名 1-Azakenpaullone
英文名称 1-Azakenpaullone
CAS 676596-65-9
分子式 C15 H10 Br N3 O
分子量 328.16
纯度 ≥98%
单位 瓶
生物活性 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。
激酶实验 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]
SMILES O=C(NC1=CC=CN=C12)CC3=C2NC4=C3C=C(Br)C=C4
靶点 GSK-3
动物实验 Cell lines: INS-1E β细胞系;Concentrations: 20 μM;Incubation Time: 4 天[4]
细胞实验 Animal Models: 雄性 NMRI小鼠;Dosages: ~500 pmol;Administration: 脑内注射[5]
数据来源文献 [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.
规格 2mg

是一种高度选择性GSK-3β抑制剂。