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237430-03-4

237430-03-4 structure
237430-03-4 structure
  • Name: Alsterpaullone
  • Chemical Name: Alsterpaullone
  • CAS Number: 237430-03-4
  • Molecular Formula: C16H11N3O3
  • Molecular Weight: 293.277
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
  • Create Date: 2018-04-05 08:00:00
  • Modify Date: 2024-01-12 18:18:24
  • 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].

Name Alsterpaullone
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
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.

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
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

~32%

237430-03-4 structure

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  2

DownStream  0

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%