Alsterpaullone (Synonyms: 9-Nitropaullone,NSC 705701) |
| Catalog No.GC15841 |
Alsterpaullone(9-Nitropaullone)은 CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E 및 CDK5/p35에 대해 IC50이 각각 35 nM, 15 nM, 200 nM 및 40 nM인 강력한 CDK 억제제입니다. Alsterpaullone은 또한 둘 다 4nM의 IC50으로 GSK-3alpha/GSK-3beta에 결합하기 위해 ATP와 경쟁합니다. Alsterpaulone은 항종양 활성을 가지며 신경퇴행성 및 증식성 장애 연구에 대한 잠재력을 가지고 있습니다. Alsterpaullon은 백혈병 세포주에서 세포 사멸을 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 237430-03-4
Sample solution is provided at 25 µL, 10mM.
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Alsterpaullone is a small molecule cyclin-dependent kinase (CDK) inhibitor [1,2].
Cyclin-dependent kinases (CDKs) are protein kinases that play important roles in the control of cell division and modulate transcription in response to several extra- and intracellular cues. Deregulation of CDKs is a hallmark of several diseases, including cancer, and drug-targeted inhibition of specific members has generated very encouraging results in clinical trials [3].
Alsterpaullone (Alp) induced apoptosis and promoted loss in clonogenicity in the Jurkat cell line. Alp activated both caspase-8 and -9, leading to cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP). Alp disrupted the activation of caspase-9 followed mitochondrial perturbation. Alp activated caspase-9 via mitochondrial perturbation [1]. Alsterpaullone regulated the cell cycle progression. Alsterpaullone inhibited HeLa cells in a time-dependent (0–72 h) and dose-dependent (0–30 μM) manner. Alsterpaullone arrested HeLa cells in G2/M prior to undergoing apoptosis via a mechanism that is involved in the regulation of various antiapoptotic genes, DNA-repair, transcription, and cell cycle progression. Alsterpaullone effectively prevented HeLa cells from entering S-phase [2].
References:
[1] Lahusen T, De Siervi A, Kunick C, et al. Alsterpaullone, a novel cyclin‐dependent kinase inhibitor, induces apoptosis by activation of caspase‐9 due to perturbation in mitochondrial membrane potential[J]. Molecular carcinogenesis, 2003, 36(4): 183-194.
[2] Cui C, Wang Y, Wang Y, et al. Alsterpaullone, a cyclin-dependent kinase inhibitor, mediated toxicity in HeLa cells through apoptosis-inducing effect[J]. Journal of analytical methods in chemistry, 2013, 2013.
[3] Malumbres M. Cyclin-dependent kinases[J]. Genome biology, 2014, 15(6): 122.
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