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Literature summary for 2.7.11.22 extracted from

  • Ali, S.; Heathcote, D.A.; Kroll, S.H.; Jogalekar, A.S.; Scheiper, B.; Patel, H.; Brackow, J.; Siwicka, A.; Fuchter, M.J.; Periyasamy, M.; Tolhurst, R.S.; Kanneganti, S.K.; Snyder, J.P.; Liotta, D.C.; Aboagye, E.O.; Barrett, A.G.; Coombes, R.C.
    The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity (2009), Cancer Res., 69, 6208-6215.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
CDK-activating kinase the CDK-activating kinase (having three subunits, CDK7, cyclin H, and MAT1) plays a critical role in regulating cell cycle by mediating the activating phosphorylation of CDK1, CDK2, CDK4, and CDK6 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BS-181 only inhibits CDK2 at concentrations lower than 1 mM, with CDK2 being inhibited 35fold less potently than CDK7 Homo sapiens
roscovitine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MCF-7 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + RNA polymerase II
-
Homo sapiens ADP + phosphorylated RNA polymerase II
-
?

Synonyms

Synonyms Comment Organism
Cdk1
-
Homo sapiens
CDK2
-
Homo sapiens
CDK4
-
Homo sapiens
Cdk5
-
Homo sapiens
cdk6
-
Homo sapiens
cdk7
-
Homo sapiens
CDK9
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens
cyclin D1 cofactor of CDK4 Homo sapiens
cyclin E cofactor of CDK2 Homo sapiens
cyclin H cofactor of CDK7 Homo sapiens
cyclin T cofactor of CDK9 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000021
-
CDK7 Homo sapiens BS-181
0.0001
-
CDK2 Homo sapiens roscovitine
0.00024
-
CDK5 Homo sapiens roscovitine
0.00051
-
CDK7 Homo sapiens roscovitine
0.00088
-
CDK2 Homo sapiens BS-181
0.0012
-
CDK9 Homo sapiens roscovitine
0.0018
-
CDK1 Homo sapiens roscovitine
0.003
-
CDK5 Homo sapiens BS-181
0.0042
-
CDK9 Homo sapiens BS-181
0.0081
-
CDK1 Homo sapiens BS-181
0.0153
-
CDK4 Homo sapiens roscovitine
0.028
-
CDK6 Homo sapiens roscovitine
0.033
-
CDK4 Homo sapiens BS-181
0.047
-
CDK6 Homo sapiens BS-181