BIBR 1532

- Overview
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    Background
    
    BIBR 1532 is a novel, specific telomerase inhibitor with IC50 of 93 nM [1].
    It has been reported that BIBR 1532 inhibited the reverse transcriptase of telomerase, hTERT, and shortened the length of the telomerase to suppress human cancer cell proliferation [1]. In pre-B acute lymphoblastic leukemia cells, BIBR1532 suppressed c-Myc and hTERT expression in a concentration-dependent manner to inhibit telomerase activity, and high doses of BIBR1532 could induce apoptosis by elevating p73, Bax/Bcl-2 and caspase-3 activation [2]. In NB4 leukemic cells, combined treatments with BIBR 1532 and arsenic trioxide suppressed cell proliferative capacity and inhibited telomerase activity probably via transcriptional suppression of c-Myc and hTERT. [4]
    
    [1]. Damm, K.; Hemmann, U.; Garin-Chesa, P.; Hauel, N.; Kauffman, I.; Priepke, H.; Niestroj, C.; Daiber, C.; Enenkel, B.; Guilliard, B.; Lauritsch, I.; Muller, E.; Pascolo, E.; Sauter, G.; Pantic, M.; Martens, U. M.; Wenz, C.; Linger, J.; Kraut, N.; Rettig, W. J.;Schnapp, A. A highly selective telomerase inhibitor limiting human cancer cell proliferation. EMBO J. 2001, 20, 6958−6968.
    [2]. Bashash D1, Ghaffari SH, Mirzaee R, Alimoghaddam K, Ghavamzadeh A. Telomerase inhibition by non-nucleosidic compound BIBR1532 causes rapid cell death in pre-B acute lymphoblastic leukemia cells. Leuk Lymphoma. 2013 Mar;54
    [4]:561-8. doi: 10.3109/10428194.2012.704034. Epub 2012 Sep 28.
    [3]. Bashash D1, Ghaffari SH, Zaker F, Kazerani M, Hezave K, Hassani S, Rostami M, Alimoghaddam K, Ghavamzadeh A. Anticancer Agents Med Chem. 2013 Sep;13(7):1115-25. BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for APL.
- Properties
  - Alternative Name
    
    2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid
    
    CAS Number
    
    321674-73-1
    
    Molecular Formula
    
    C21H17NO3
    
    Molecular Weight
    
    331.36
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥15.65 mg/mL in DMSO; ≥2.36 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Doğan F, Özateş NP, et al. "Investigation of the effect of telomerase inhibitor BIBR1532 on breast cancer and breast cancer stem cells." J Cell Biochem. 2018 Oct 28. PMID:30368861
    2. Biray Avci C, Dogan F, et al."Effects of telomerase inhibitor on epigenetic chromatin modification enzymes in malignancies." J Cell Biochem. 2018 Aug 26. PMID:30145821

BIBR 1532

Background

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