Reaction Details
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Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Ligand
BDBM5774
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition assay
pH
8.0000±n/a
Temperature
303.1500±n/a K
IC50
32±n/a nM
Citation
Misra, RN; Xiao, H; Rawlins, DB; Shan, W; Kellar, KA; Mulheron, JG; Sack, JS; Tokarski, JS; Kimball, SD; Webster, KR 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett 13:2405-8 (2003) [PubMed] Article Target
Name:
Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Synonyms:
cdk1 | CDK1/B | CDK1/Cyclin B | CDK1/CyclinB | Cyclin B/Dependent Kinase 1 (CDK1) | Cyclin-Dependent Kinase 1 (CDK1) | Cyclin-dependent kinase 1/cyclin B1 | Cyclin-dependent kinase/G2/mitotic-specific cyclin 1
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
CDK1/Cyclin B 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 1
Synonyms:
Cell division control protein 2 homolog | Cell division protein kinase 1 | Cyclin-dependent kinase 1 (CDK1) | p34 protein kinase | CDK1_HUMAN | CDK1 | CDC2 | CDC28A | CDKN1 | P34CDC2
Type:
Enzyme Subunit
Mol. Mass.:
34101.08
Organism:
Human
Description:
P06493
Residue:
297
Sequence:
MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRHPNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCHSRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSARYSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNTFPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM
Component 2
Name:
G2/mitotic-specific cyclin-B1
Synonyms:
CCNB1_HUMAN | CCNB1 | CCNB
Type:
Enzyme Subunit
Mol. Mass.:
48340.95
Organism:
Human
Description:
P14635
Residue:
433
Sequence:
MALRVTRNSKINAENKAKINMAGAKRVPTAPAATSKPGLRPRTALGDIGNKVSEQLQAKMPMKKEAKPSATGKVIDKKLPKPLEKVPMLVPVPVSEPVPEPEPEPEPEPVKEEKLSPEPILVDTASPSPMETSGCAPAEEDLCQAFSDVILAVNDVDAEDGADPNLCSEYVKDIYAYLRQLEEEQAVRPKYLLGREVTGNMRAILIDWLVQVQMKFRLLQETMYMTVSIIDRFMQNNCVPKKMLQLVGVTAMFIASKYEEMYPPEIGDFAFVTDNTYTKHQIRQMEMKILRALNFGLGRPLPLHFLRRASKIGEVDVEQHTLAKYLMELTMLDYDMVHFPPSQIAAGAFCLALKILDNGEWTPTLQHYLSYTEESLLPVMQHLAKNVVMVNQGLTKHMTVKNKYATSKHAKISTLPQLNSALVQDLAKAVAKV
Inhibitor
Name:
BDBM5774
Synonyms:
4-butoxy-5-[(2,6-difluorophenyl)carbonyl]-1H-pyrazolo[3,4-b]pyridine | pyrazolo[3,4-b]pyridine deriv. | SQ-67563 Analog 21f
Type:
Small organic molecule
Emp. Form.:
C17H15F2N3O2
Mol. Mass.:
331.11
SMILES:
CCCCOc1c(cnc2[nH]ncc12)C(=O)c1c(F)cccc1F
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bovine
Description:
25 uM ATP/0.2 uCi[gamma-33P] as co-substrate.
Residue:
3
Sequence:
NA
