Reaction Details
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Cyclin-A2 [171-432]/Cyclin-dependent kinase 2
Ligand
BDBM5485
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
Ki
12000±3000 nM
Comments
To obtain Ki value, the assay was performed in the absence of inhibitor and at two fixed inhibitor concentrations, 25 and 50 uM, with ATP concentrations ranging from 6.25 to 800 uM. Data were fitted to the Michaelis-Menten equation using unweighted nonlinear least squares regression.
Citation
Arris, CE; Boyle, FT; Calvert, AH; Curtin, NJ; Endicott, JA; Garman, EF; Gibson, AE; Golding, BT; Grant, S; Griffin, RJ; Jewsbury, P; Johnson, LN; Lawrie, AM; Newell, DR; Noble, ME; Sausville, EA; Schultz, R; Yu, 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 More Info.:
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:
BDBM5485
Synonyms:
6-(cyclohexylmethoxy)-9H-purin-2-amine | CHEMBL269881 | NU2058
Type:
Small organic molecule
Emp. Form.:
C12H17N5O
Mol. Mass.:
247.2963
SMILES:
Nc1nc(OCC2CCCCC2)c2[nH]cnc2n1
Structure:
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