Reaction Details |
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Target | Cyclin-T1/Cyclin-dependent kinase 9 |
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Ligand | BDBM7533 |
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Substrate/Competitor | Retinoblastoma (Rb) |
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Meas. Tech. | CDK Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 303.15±n/a K |
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IC50 | 230±n/a nM |
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Citation | Popowycz, F; Fournet, G; Schneider, C; Bettayeb, K; Ferandin, Y; Lamigeon, C; Tirado, OM; Mateo-Lozano, S; Notario, V; Colas, P; Bernard, P; Meijer, L; Joseph, B Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue. J Med Chem52:655-63 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Cyclin-T1/Cyclin-dependent kinase 9 |
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Name: | Cyclin-T1/Cyclin-dependent kinase 9 |
Synonyms: | CDK9/ Cyclin-T1 | CDK9/CycT1 | CDK9/Cyclin T | CDK9/Cyclin T1 | Cyclin T1/dependent kinase 9 | Cyclin-Dependent Kinase 9 (CDK9) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cyclin-T1 |
Synonyms: | CCNT1 | CCNT1_HUMAN | CycT | CycT1 | Cyclin T | Cyclin T1 | Cyclin-T |
Type: | Enzyme Subunit |
Mol. Mass.: | 80712.40 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 726 |
Sequence: | MEGERKNNNKRWYFTREQLENSPSRRFGVDPDKELSYRQQAANLLQDMGQRLNVSQLTIN
TAIVYMHRFYMIQSFTQFPGNSVAPAALFLAAKVEEQPKKLEHVIKVAHTCLHPQESLPD
TRSEAYLQQVQDLVILESIILQTLGFELTIDHPHTHVVKCTQLVRASKDLAQTSYFMATN
SLHLTTFSLQYTPPVVACVCIHLACKWSNWEIPVSTDGKHWWEYVDATVTLELLDELTHE
FLQILEKTPNRLKRIWNWRACEAAKKTKADDRGTDEKTSEQTILNMISQSSSDTTIAGLM
SMSTSTTSAVPSLPVSEESSSNLTSVEMLPGKRWLSSQPSFKLEPTQGHRTSENLALTGV
DHSLPQDGSNAFISQKQNSKSVPSAKVSLKEYRAKHAEELAAQKRQLENMEANVKSQYAY
AAQNLLSHHDSHSSVILKMPIEGSENPERPFLEKADKTALKMRIPVAGGDKAASSKPEEI
KMRIKVHAAADKHNSVEDSVTKSREHKEKHKTHPSNHHHHHNHHSHKHSHSQLPVGTGNK
RPGDPKHSSQTSNLAHKTYSLSSSFSSSSSTRKRGPSEETGGAVFDHPAKIAKSTKSSSL
NFSFPSLPTMGQMPGHSSDTSGLSFSQPSCKTRVPHSKLDKGPTGANGHNTTQTIDYQDT
VNMLHSLLSAQGVQPTQPTAFEFVRPYSDYLNPRSGGISSRSGNTDKPRPPPLPSEPPPP
LPPLPK
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Component 2 |
Name: | Cyclin-dependent kinase 9 |
Synonyms: | C-2K | CDC2L4 | CDK9 | CDK9_HUMAN | Cell division cycle 2-like protein kinase 4 | Cell division protein kinase 9 | Cyclin-Dependent Kinase 9 (CDK9) | Cyclin-dependent kinase 9 (CDK9) | Serine/threonine-protein kinase PITALRE | TAK | Tat-associated kinase complex catalytic subunit |
Type: | Enzyme Subunit |
Mol. Mass.: | 42789.13 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 372 |
Sequence: | MAKQYDSVECPFCDEVSKYEKLAKIGQGTFGEVFKARHRKTGQKVALKKVLMENEKEGFP
ITALREIKILQLLKHENVVNLIEICRTKASPYNRCKGSIYLVFDFCEHDLAGLLSNVLVK
FTLSEIKRVMQMLLNGLYYIHRNKILHRDMKAANVLITRDGVLKLADFGLARAFSLAKNS
QPNRYTNRVVTLWYRPPELLLGERDYGPPIDLWGAGCIMAEMWTRSPIMQGNTEQHQLAL
ISQLCGSITPEVWPNVDNYELYEKLELVKGQKRKVKDRLKAYVRDPYALDLIDKLLVLDP
AQRIDSDDALNHDFFWSDPMPSDLKGMLSTHLTSMFEYLAPPRRKGSQITQQSTNQSRNP
ATTNQTEFERVF
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BDBM7533 |
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Retinoblastoma (Rb) |
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Name: | Retinoblastoma (Rb) |
Synonyms: | RB1 | RB_HUMAN | Rb | Retinoblastoma-associated protein | p105-Rb | pRB | pp110 |
Type: | Other Protein Type |
Mol. Mass.: | 17470.92 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant fusion protein containing the C-terminal fragment (residues 773-928) |
Residue: | 156 |
Sequence: | STRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRIL
VSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLP
GESKFQQKLAEMTSTRTRMQKQKMNDSMDTSNKEEK
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