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Alsterpaullone CDKs and GSK3β inhibitor

Catalog No.B7855
Size Price Stock Qty
1mg
$61.00
In stock
5mg
$273.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Alsterpaullone

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Chemical Properties

Cas No. 237430-03-4 SDF Download SDF
Synonyms 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
Solubility Soluble in DMSO Storage Store at -20°C
Physical Appearance Yellow to brown powder Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.