Target
Cyclin-A2 [171-432]/Cyclin-dependent kinase 2
Ligand
BDBM5565
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
>100000±n/a nM
Citation
 Arris, CEBoyle, FTCalvert, AHCurtin, NJEndicott, JAGarman, EFGibson, AEGolding, BTGrant, SGriffin, RJJewsbury, PJohnson, LNLawrie, AMNewell, DRNoble, MESausville, EASchultz, RYu, W Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem 43:2797-804 (2000) [PubMed]  Article 
Target
Name:
Cyclin-A2 [171-432]/Cyclin-dependent kinase 2
Synonyms:
CDK2/cyclin A3 | Cyclin-Dependent Kinase 2 (CDK2) | p33cdk2/cyclin A3
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
Binary complex of CDK2-cyclin A3 was formed by adding cyclin A3 in slight molar excess to the CDK2 subunit and purified by Superdex 75 gel filtration chromatography.
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 2
Synonyms:
CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase
Type:
Enzyme Subunit
Mol. Mass.:
33938.17
Organism:
Homo sapiens (Human)
Description:
P24941
Residue:
298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
  
Component 2
Name:
Cyclin-A2 [171-432]
Synonyms:
CCN1 | CCNA | CCNA2 | CCNA2_HUMAN | cyclin A2
Type:
Enzyme Subunit
Mol. Mass.:
30018.91
Organism:
Homo sapiens (Human)
Description:
cyclin A2 is a c-terminal cyclin A fragment encoding residues 171-432.
Residue:
262
Sequence:
SVNEVPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHGVSLLNPPETLNL
  
Inhibitor
Name:
BDBM5565
Synonyms:
6-(cyclohexylmethoxy)-9-methyl-9H-purin-2-amine | NU6052 | O6-Cyclohexylmethyl-N9-methylguanine
Type:
Small organic molecule
Emp. Form.:
C13H19N5O
Mol. Mass.:
261.3229
SMILES:
Cn1cnc2c(OCC3CCCCC3)nc(N)nc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
Sigma Type IIIS
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
12.5 uM ATP as co-substrate.
Residue:
3
Sequence:
NA