NU 6140

Names

[ Name ]:
NU 6140

[Synonym ]:
Cdk2 Inhibitor IV,NU6140
HMS3229E18
IN1369

Biological Activity

[Description]:

NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs[1]. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively[2]. Anti-cancer activity[1][2].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Aurora Kinase

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

[Target]

cdk2-cyclin A:0.41 μM (IC50)

CDK1-Cyclin B:6.6 μM (IC50)

CDK4-Cyclin D:5.5 μM (IC50)

cdk5-p25:15 μM (IC50)

cdk7-cyclin H:3.9 μM (IC50)

Aurora A:67 nM (IC50)

Aurora B:35 nM (IC50)

[In Vitro]

NU6140 is less active on CDK1-cyclin B, CDK4-cyclin D, CDK5-p25 and CDK7-cyclin H, with IC50s of 0.41, 6.6, 5.5, 15 and 3.9 μM, respectively[1]. NU6140 increases catalytic activity of capase-9 and capase-3, causes increase in the sub-G1 apoptotic cell population[1].

[References]

[1]. Pennati M, et al. Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₃₀N₆O₂

[ Molecular Weight ]:
422.52

[ Exact Mass ]:
422.24300

[ PSA ]:
96.03000

[ LogP ]:
4.61060

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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