Alsterpaullone

Modify Date: 2024-01-12 18:18:24

Alsterpaullone Structure
Alsterpaullone structure
Common Name Alsterpaullone
CAS Number 237430-03-4 Molecular Weight 293.277
Density 1.5±0.1 g/cm3 Boiling Point 651.5±45.0 °C at 760 mmHg
Molecular Formula C16H11N3O3 Melting Point N/A
MSDS Chinese USA Flash Point 347.8±28.7 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of Alsterpaullone


Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to glycogen synthase kinase-3 alpha/beta (GSK-3alpha/GSK-3beta) with an IC50 of 4 nM, with antitumor activity and potential for the treatment of neurodegenerative and proliferative disorders[1].

 Names

Name Alsterpaullone
Synonym More Synonyms

 Alsterpaullone Biological Activity

Description Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to glycogen synthase kinase-3 alpha/beta (GSK-3alpha/GSK-3beta) with an IC50 of 4 nM, with antitumor activity and potential for the treatment of neurodegenerative and proliferative disorders[1].
Related Catalog
Target

Cdk1/cyclin B:35 nM (IC50)

cdk2/cyclin A:15 nM (IC50)

CDK2/Cyc E:200 nM (IC50)

CDK5/p35:40 nM (IC50)

GSK-3α:4 (IC50)

GSK-3β:4 nM (IC50)

References

[1]. Leost M, et al. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000 Oct;267(19):5983-94.

[2]. Lahusen T, et al. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003 Apr;36(4):183-94.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 651.5±45.0 °C at 760 mmHg
Molecular Formula C16H11N3O3
Molecular Weight 293.277
Flash Point 347.8±28.7 °C
Exact Mass 293.080048
PSA 90.71000
LogP 3.55
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.738

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi: Irritant;
Risk Phrases R36/37/38
Safety Phrases 26-36
RIDADR NONH for all modes of transport
HS Code 2933990090

 Synthetic Route

~32%

Alsterpaullone Structure

Alsterpaullone

CAS#:237430-03-4

Literature: Zaharevitz, Daniel W.; Gussio, Rick P.; Jalluri, Ravi K.; Sausville, Edward A.; Kunick, Conrad; Meijer, Laurent Patent: US2002/42412 A1, 2002 ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles4

More Articles
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.

J. Med. Chem. 42 , 2909, (1999)

The paullones represent a novel class of small molecule cyclin-dependent kinase (CDK) inhibitors. To investigate structure-activity relationships and to develop paullones with antitumor activity, deri...

Evidence for antimanic efficacy of glycogen synthase kinase-3 (GSK3) inhibitors in a strain-specific model of acute mania.

Int. J. Neuropsychopharmacol. 14 , 1051-67, (2011)

There is a growing body of evidence suggesting that animal models can be developed to probe the specific domains of bipolar disorder (BD) using the endophenotype approach. Here we tested clinically ac...

Induction of canonical Wnt signaling by alsterpaullone is sufficient for oral tissue fate during regeneration and embryogenesis in Nematostella vectensis.

Dev. Dyn. 240 , 2673-9, (2011)

Although regeneration is widespread among metazoa, the molecular mechanisms have been studied in only a handful of taxa. Of these taxa, fewer still are amenable to studies of embryogenesis. Our unders...

 Synonyms

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