Merck, 5088390001, Telomerase Inhibitor X, BIBR1532

General description
A cell-permeable benzoic acid based compound that acts as a selective, highly potent, non-nucleotide competitive inhibitor of the catalytic activity of telomerase (IC₅₀ = 93 nM in HeLa cells nuclear extracts). Also shown to be effective against recombinant, affinity purified telomerase. Blocks the growth and proliferation of HeLa cells (~ 20 µM) by inducing apoptosis. The inhibition appears to be more prominent in TEL patch mutant cell lines. Causes a continuous erosion of telomeres in multiple human cancer cell lines. Does not affect the activity of DNA and RNA polymerases in any significant manner.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Teomerase
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Damm, K., et al. 2001. The. EMBO J.20, 6958.
Pascolo, E., et al. 2002. J. Biol. Chem.277,15566.
Nakashima, M., et al. 2013. J. Biol. Chem.288, 33171.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)