Alsteropaullone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Alsteropaullone (9-Nitropaullone, NSC 705701) 是 kenpaullone 的衍生物，是 CDK 和 GSK3β 的 ATP 竞争性抑制剂，抑制 Cdk1/cyclin B、Cdk2/cyclin A、Cdk2/cyclin E 和 Cdk5/p25，IC50 分别为 35、15、 200 和 40 nM。

Alsteropaullone (9-Nitropaullone, NSC 705701) is a derivative of kenpaullone, ATP-competitive inhibitor of CDKs and GSK3β, inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E and Cdk5/p25 with IC50 of 35, 15, 200 and 40 nM; exhibits specific antitumor activity against Group 3 medulloblastomas, causes inhibition of cell cycle-related genes, and down-regulation of MYC; inhibits the cytosolic degradation of β-catenin to alter the canonical Wnt signaling pathway in primary axis patterning, reduces tau phosphorylation.

Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line.Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too. Alsterpaullone (20?μM) induces cell death depending on caspase activity. Cell Viability Assay Cell Line:HeLa cells Concentration:5, 10, 15, 20, 25, 30 μMIncubation Time:48 and 72 hoursResult:The growth of HeLa cells was inhibited in a dose-dependent manner for 48?h and 72?h ranging from 0 to 30?μM.Apoptosis Analysis Cell Line:Jurkat cell line Concentration:0.3, 1, 3 μM Incubation Time:8 hours Result:Induced dose-dependent apoptosis. 1 μM was sufficient to cause apoptosis, 3 μM demonstrated maximal apoptotic effects.Western Blot Analysis Cell Line:HeLa cells Concentration:2, 4, 6, 12, 24 hours Incubation Time:8 hours Result:The cleavage of PARP started at 4?h, while the activation of caspase-3 occurred at 2?h.

Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts. Animal Model:5-6 week old athymic nude mice Dosage:30 mg/kg Administration : Subcutaneous injections, daily for 2 weeks Result:Antitumor effect in Group 3 medulloblastomas.

9-Nitropaullone | NSC 705701

Angiogenesis

CDK

CDK

——

——

237430-03-4

293.3

C16H11N3O3

>98% (HPLC)

——

O=C1NC2=CC=CC=C2C(NC3=C4C=C([N+]([O-])=O)C=C3)=C4C1

7,12-dihydro-9-nitro-indolo[3,2-d][1]benzazepin-6(5H)-one

(-20℃)

With Ice Pack

≥ 2 years