A potent telomerase inhibitor
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BIBR 1532

Item No. 16608

Technical Information
Formal Name
2-[[(2E)-3-(2-naphthalenyl)-1-oxo-2-buten-1-yl]amino]-benzoic acid
CAS Number
321674-73-1
Synonyms
  • Telomerase Inhibitor X
Molecular Formula
C21H17NO3
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
214, 243, 268, 303, 320 nm
SMILES
C/C(C1=CC2=CC=CC=C2C=C1)=C\C(NC3=C(C=CC=C3)C(O)=O)=O
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BIBR 1532 is a mixed-type non-competitive inhibitor of telomerase (IC50 = 93 nM) that has little effect on several mammalian DNA and RNA polymerases, bacterial DNA helicase, or HIV-1 reverse transcriptase.1,2,3 It specifically targets the telomerase reverse transcriptase catalytic subunit, TERT.2,4 Through its effects on telomerase, BIBR 1532 induces senescence or apoptosis in cancer cells.1,5 Apoptosis in triple negative breast cancer cells induced by BIBR 1532 is potentiated by glucose restriction.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Damm, K., Hemmann, U., Garin-Chesa, P., et alA highly selective telomerase inhibitor limiting human cancer cell proliferation. EMBO J. 20(24), 6958-6968 (2014).

    2. Pascolo, E., Wenz, C., Lingner, J., et alMechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. The Journal of Biological Chemisty 277(18), 15566-15572 (2002).

    3. Piotrowska, K., Kleideiter, E., Mürdter, T.E., et alOptimization of the TRAP assay to evaluate specificity of telomerase inhibitors. Lab. Invest. 85(12), 1565-1569 (2005).

    4. Phatak, P., and Burger, A.M. Telomerase and its potential for therapeutic intervention. Br. J. Pharmacol. 152(7), 1003-1011 (2007).

    5. Wardi, L., Alaaeddine, N., Raad, I., et alGlucose restriction decreases telomerase activity and enhances its inhibitor response on breast cancer cells: Possible extra-telomerase role of BIBR 1532. Cancer Cell Int. 14, 60 (2014).