Description
Key facts
CAS number:284028-89-3,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:312.31 g/mol,
Molecular formula:C14H11F3N2OS,
Nature:Synthetic,
Solubility:Soluble in DMSO to 25 mM,
Biological description:Potent tankyrase (TNKS) inhibitor. Inhibitor of Wnt/β-catenin signaling. (IC50 values are 11 and 4 nM for TNKS1 and 2, respectively). Inhibits TNKS PARP activity. Selectivity over other PARP enzymes and CRE, NK-κB and TGF-β.,
Canonical smiles:OC1=NC(C2=CC=C(C(F)(F)F)C=C2)=NC3=C1CSCC3,
IUPAC Name:3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Tankyrase also known as TNKS and tankyrase-1 is an enzyme belonging to the poly(ADP-ribose) polymerase (PARP) family with a molecular mass of about 142 kDa. It is expressed in various tissues including brain heart and liver as well as in certain types of cancer cells. Mechanically tankyrase catalyzes the addition of ADP-ribose polymers to protein substrates a process known as poly(ADP-ribosyl)ation. This activity modulates the stability localization or interactions of target proteins.
Biological function summary
Tankyrase functions in diverse cellular processes. It participates in telomere maintenance by ADP-ribosylating TRF1 a telomere-binding protein leading to TRF1's disassembly from telomeres. Moreover tankyrase acts in the regulation of Wnt/β-catenin signaling where it associates with components like AXIN influencing the stability of the β-catenin destruction complex. Tankyrase can also be part of larger protein complexes such as the shelterin complex playing a role in safeguarding chromosome ends.
Pathways
Tankyrase integrates into key signaling networks. In the Wnt/β-catenin pathway tankyrase's interaction with AXIN controls the availability of β-catenin an important transcription co-activator in cell proliferation and differentiation. This enzyme also connects with the telomere maintenance pathway engaging TRF1 and contributing to telomere elongation and stability. Through these pathways tankyrase engages in processes vital for cell growth and genome integrity.
Tankyrase is implicated in cancer and heritable disorders of telomere dysfunction. Abnormal tankyrase activity correlates with increased β-catenin levels promoting oncogenesis in colorectal and other cancers. Additionally disruptions in tankyrase-mediated telomere regulation can lead to conditions like dyskeratosis congenita. Tankyrase links with proteins such as β-catenin in cancer while in telomere-related disorders it connects with TRF1 indicating its significance in maintaining cellular homeostasis.
