Alsterpaullone

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Alsterpaullone

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

237430-03-4

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议

产品介绍

Alsterpaullon (9-Nitropaullone) 是一种有效的 CDK 抑制剂，对 CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p35 的 IC50 分别为 35 nM、15 nM、200 nM 和 40 nM。 Alsterpaullon 还与 ATP 竞争结合 GSK-3alpha/GSK-3beta，IC50 均为 4 nM。 Alsterpaullone 具有抗肿瘤活性，并具有研究神经退行性和增殖性疾病的潜力。 Alsterpaullone 在白血病细胞系中诱导细胞凋亡。

Cas No.	237430-03-4
别名	阿特波龙,9-Nitropaullone,NSC 705701
化学名	9-nitro-7,12-dihydrobenzo[2,3]azepino[4,5-b]indol-6(5H)-one
Canonical SMILES	O=C1CC2=C(C3=CC=CC=C3N1)NC4=C2C=C(C=C4)[N+]([O-])=O
分子式	C₁₆H₁₁N₃O₃
分子量	293.28
溶解度	DMF: 3 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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.