" /> Tambiciclib - CISMeF





Preferred Label : Tambiciclib;

NCIt synonyms : CDK9 Inhibitor GFH009;

NCIt definition : A selective inhibitor of the serine/threonine 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, tambiciclib targets, binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II, leading to the inhibition of gene transcription of various anti-apoptotic proteins. This induces cell cycle arrest and apoptosis and prevents tumor cell proliferation. CDK9 regulates elongation of transcription through phosphorylation of RNA Pol II at serine 2 (p-Ser2-RNAPII). It is upregulated in various tumor cell types and 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 : XDZ7VK8CXC;

CAS number : 2247481-08-7;

Molecule name : SLS 009; GFH-009; SLS-009; GFH 009;

NCI Metathesaurus CUI : CL1929144;

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30/07/2025


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