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Target
Cyclin-A2/Cyclin-dependent kinase 2
Ligand
BDBM7718
Substrate
Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
IC50
3.0±n/a nM
Citation
Bramson, HN; Corona, J; Davis, ST; Dickerson, SH; Edelstein, M; Frye, SV; Gampe, RT; Harris, PA; Hassell, A; Holmes, WD; Hunter, RN; Lackey, KE; Lovejoy, B; Luzzio, MJ; Montana, V; Rocque, WJ; Rusnak, D; Shewchuk, L; Veal, JM; Walker, DH; Kuyper, LF Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis. J Med Chem 44:4339-58 (2001) [PubMed] Article
More Info.:
Target
Name:
Cyclin-A2/Cyclin-dependent kinase 2
Synonyms:
CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | CDK2/Cyclin A2 | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-Dependent Kinase 2 (CDK2A)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus.
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:
Human
Description:
P24941
Residue:
298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
Component 2
Name:
Cyclin-A2
Synonyms:
CCN1 | CCNA | CCNA1 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A
Type:
Enzyme Subunit
Mol. Mass.:
48550.19
Organism:
Human
Description:
P20248
Residue:
432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRGLAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKIEREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHGVSLLNPPETLNL
Inhibitor
Name:
BDBM7718
Synonyms:
2-methylpropyl (3Z)-2-oxo-3-{[(4-sulfamoylphenyl)amino]methylidene}-2,3-dihydro-1H-indole-5-carboxylate | Isobutyl 3-{[4-(aminosulfonyl)anilino]methylene}-2-oxo-2,3-dihydro-1H-indole-5-carboxylate | Oxindole-Based Inhibitor 54
Type:
Small organic molecule
Emp. Form.:
C20H21N3O5S
Mol. Mass.:
415.463
SMILES:
CC(C)COC(=O)c1ccc2NC(=O)C(C=Nc3ccc(cc3)S(N)(=O)=O)c2c1 |w:15.14|
Substrate
Name:
Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
5198.94
Organism:
n/a
Description:
n/a
Residue:
46
Sequence:
ITINAMINHEYLALAARGARGPRMETSERPRLYSLYSLYSALACNH