Reaction Details
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Cyclin-A2 [171-432]/Cyclin-dependent kinase 2
Ligand
BDBM5566
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
Ki
1300±200 nM
Comments
To obtain Ki value, the assay was performed in the absence of inhibitor and at two fixed inhibitor concentrations, 5 and 10 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:
BDBM5566
Synonyms:
2,6-Diamino-4-cyclohexylmethoxy-5-nitrosopyrimidine | 6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine | NU6027 | pyrimidine deriv.
Type:
Small organic molecule
Emp. Form.:
C11H17N5O2
Mol. Mass.:
251.285
SMILES:
Nc1nc(N)c(N=O)c(OCC2CCCCC2)n1
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