NCIt definition : An inhibitor of cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA
polymerase II (RNA Pol II) elongation factor positive transcription elongation factor
b (PTEF- b; PTEFb), with potential antineoplastic activity. Upon administration, enitociclib
binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing
PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription
of various anti-apoptotic proteins. This may cause cell cycle arrest and induce apoptosis,
which may lead to a reduction in tumor cell proliferation. The protein complex PTEF-b,
a heterodimer consisting of CDK9 and a regulatory cyclin subunit of the T family,
is over-activated in various tumor cell types; it plays a key role in the regulation
of Pol II-mediated transcription of anti-apoptotic proteins. Tumor cells are dependent
on anti-apoptotic proteins for their survival.;
UNII : 1255AT22ZJ;
CAS number : 1610408-97-3;
Molecule name : BAY1251152; BAY 1251152; VIP-152; VIP 152;