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Alsterpaullone (Synonyms: 9-Nitropaullone,NSC 705701)

Katalog-Nr.GC15841

Alsterpaullon (9-Nitropaullon) ist ein potenter CDK-Inhibitor mit IC50-Werten von 35 nM, 15 nM, 200 nM und 40 nM fÜr CDK1/Cyclin B, CDK2/Cyclin A, CDK2/Cyclin E bzw. CDK5/p35. Alsterpaullon konkurriert auch mit ATP um die Bindung an GSK-3alpha/GSK-3beta mit IC50-Werten von jeweils 4 nM. Alsterpaullon hat AntitumoraktivitÄt und besitzt Potenzial fÜr die Untersuchung von neurodegenerativen und proliferativen Erkrankungen. Alsterpaullon induziert Apoptose in LeukÄmie-Zelllinien.

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Alsterpaullone Chemische Struktur

Cas No.: 237430-03-4

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Sample solution is provided at 25 µL, 10mM.

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Background

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.

Chemical Properties

Cas No. 237430-03-4 SDF
Überlieferungen 9-Nitropaullone,NSC 705701
Chemical Name 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
Formula C16H11N3O3 M.Wt 293.28
Löslichkeit DMF: 3 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.4097 mL 17.0486 mL 34.0971 mL
5 mM 0.6819 mL 3.4097 mL 6.8194 mL
10 mM 0.341 mL 1.7049 mL 3.4097 mL
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