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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM6780
Substrate
ING Peptide
Meas. Tech.
CDK Kinase Inhibition Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
2140±n/a nM
Citation
 Sanchez-Martinez, C; Shih, C; Zhu, G; Li, T; Brooks, HB; Patel, BK; Schultz, RM; DeHahn, TB; Spencer, CD; Watkins, SA; Ogg, CA; Considine, E; Dempsey, JA; Zhang, F Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. Bioorg Med Chem Lett 13:3841-6 (2003) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Synonyms:
CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1 | Cyclin-dependent kinase 4/cyclin D1
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
CDK4/D1 complexes were purified from insect cells co-infected with baculovirus vectors containing each of the components.
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 4
Synonyms:
CDK4 | CDK4_HUMAN | Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | PSK-J3
Type:
Enzyme Subunit
Mol. Mass.:
33731.96
Organism:
Homo sapiens (Human)
Description:
P11802
Residue:
303
Sequence:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALLRRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDLMRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWYRAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPRDVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEGNPE
  
Component 2
Name:
G1/S-specific cyclin-D1
Synonyms:
B-cell lymphoma 1 protein | BCL-1 | BCL-1 oncogene | BCL1 | CCND1 | CCND1_HUMAN | PRAD1 | PRAD1 oncogene
Type:
Enzyme Subunit
Mol. Mass.:
33717.70
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
  
Inhibitor
Name:
BDBM6780
Synonyms:
3-[1-(2,3-dihydroxypropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | bis-indolylmaleimide deriv. 8j
Type:
Small organic molecule
Emp. Form.:
C24H21N3O4
Mol. Mass.:
415.4412
SMILES:
Cn1cc(C2=C(C(=O)NC2=O)c2cn(CC(O)CO)c3ccccc23)c2ccccc12 |t:4|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
ING Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1341.50
Organism:
n/a
Description:
amino acid residues 246-257 from human retinoblastoma 1 protein.
Residue:
12
Sequence:
INGSPRTPRRGQ