5.08839

Telomerase Inhibitor X, BIBR1532

• Synonym(s): Telomerase Inhibitor X, BIBR1532, BIBR 1532, BIBR-1532
• Empirical Formula (Hill Notation): C₂₁H₁₇NO₃
• CAS Number: 321674-73-1
• Molecular Weight: 331.36
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• potency: 93 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C21H17NO3/c1-14(16-11-10-15-6-2-3-7-17(15)13-16)12-20(23)22-19-9-5-4-8-18(19)21(24)25/h2-13H,1H3,(H,22,23)(H,24,25)/b14-12+
• InChI key: PGFQXGLPJUCTOI-WYMLVPIESA-N

Description

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.

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable