Paullone CAS: 142273-18-5
MF: C16H12N2O
MW: 248.28
A potent inhibitor of Cdk.

Paullone (CAS 142273-18-5)

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アプリケーション: Paullone is a potent inhibitor of Cdk
CAS 番号: 142273-18-5
Molecular Weight: 248.28
Molecular Formula: C16H12N2O
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* Refer to Certificate of Analysis for lot specific data (including water content).

Paullone is a potent inhibitor of Cdk (cyclin-dependent kinases), which are involved in the regulation of the cell cycle.


参考文献

1. Kamb, A., et al., 1998. Cyclin-dependent kinase inhibitors and human cancer. Current topics in microbiology and immunology. 227(): 139-48. PMID: 9479829
2. Schultz, C., et al., 1999. Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. Journal of medicinal chemistry. 42(15): 2909-19. PMID: 10425100
3. Lahusen, Tyler., et al., 2003. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Molecular carcinogenesis. 36(4): 183-94. PMID: 12669310
4. Kunick, Conrad., et al., 2005. Structure-aided optimization of kinase inhibitors derived from alsterpaullone. Chembiochem : a European journal of chemical biology. 6(3): 541-9. PMID: 15696597

Physical State :
Solid
Solubility :
Soluble in methanol, DMSO, and DMF.
保存方法 :
Store at room temperature
Melting Point :
212.71°C (Predicted; Mean or Weighted)
Boiling Point :
571.19° C at 760 mmHg (Predicted)
Density :
1.32 g/cm3
Refractive Index :
n20D 1.72
IC50 :
Cyclin-dependent kinase 9: IC50 = 810 nM (human); Glycogen synthase kinase-3 beta: IC50 = 620 nM (human); Cyclin T1: IC50 = 810 nM (human); Glycogen synthase kinase-3 beta: IC50 = 100 nM (human); Glutamate NMDA receptor: IC50 = >1000 nM (Rattus norvegicus); Serotonin 1d (5-HT1d) receptor: IC50 = >1000 nM (Rattus norvegicus); Beta-2 adrenergic receptor: IC50 = >1000 nM (Canis lupus familiaris Multiple homologous proteins); Alpha-1a adrenergic receptor: IC50 = >1000 nM (Rattus norvegicus)
pK Values :
pKb: 1.47
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
PubChem CID :
369401
MDL Number :
MFCD18252383
SMILES :
C1C2=C(C3=CC=CC=C3NC1=O)NC4=CC=CC=C24

Download SDS (MSDS)

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Paullone (CAS 142273-18-5)  参考文献

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引用 1 to 2 of 2 合計

PMID: # 33472062  Kubota, M.|Scheibinger, M.|Jan, TA.|Heller, S.| et al. 2021. Cell Rep. 34: 108646.

PMID: # 29046299  Lee, HW. et al. 2017. Am. J. Physiol. Renal Physiol. 7: ajprenal.00338.2017.

引用 1 to 2 of 2 合計
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