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Alsterpaullone

Cat. No. M13594
Alsterpaullone Structure
Synonym:

9-Nitropaullone; NSC 705701

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Biological Activity

Alsterpaullone (9-Nitropaullone) is a potent 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 GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.

Chemical Information
Molecular Weight 293.28
CAS Number 237430-03-4
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Takahiro Watanabe, et al. Cancer Sci. Antitumor activity of cyclin-dependent kinase inhibitor alsterpaullone in Epstein-Barr virus-associated lymphoproliferative disorders

[2] Peng Yin, et al. Oncol Lett. Alsterpaullone induces apoptosis of HepG2 cells via a p38 mitogen-activated protein kinase signaling pathway

[3] Jiancai Wang, et al. Front Cell Neurosci. GSK-3β Inhibitor Alsterpaullone Attenuates MPP +-Induced Cell Damage in a c-Myc-Dependent Manner in SH-SY5Y Cells

[4] Claudia C Faria, et al. Oncotarget. Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma

[5] Chunying Cui, et al. J Anal Methods Chem. Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect

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Keywords: Alsterpaullone, 9-Nitropaullone; NSC 705701 supplier, CDK, inhibitors, activators


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