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BIBR 1532
- Soluble in DMSO
- MF: C21H17NO3
- MW: 331.36
Description
Potent and selective inhibitor of native and recombinant human telomerase (IC50 values of ca. 100 nM), capable of inducing senescence in human cancer cells. BIBR1532 is a mixed-type non-competitive inhibitor of the human telomerase reverse transcriptase and human telomerase RNA components with similar potency primarily by interfering with the processivity of the enzyme. BIBR 1532 defines a novel class of mixed-type non-competitive telomerase inhibitor with mechanistic similarities to non-nucleosidic inhibitors of HIV1 reverse transcriptase.
More Information
| Parent CAS No. | 321674-73-1 |
|---|---|
| Chemical Name | (E)-2-(3-(Naphthalen-2-yl)but-2-enamido)benzoic acid |
| SMILES | C1C=C2C=C(/C(/C)=C/C(=O)NC3C=CC=CC=3C(=O)O)C=CC2=CC=1 |
| MFCD | N.A. |
| InChi | 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+ |
| InChiKey | PGFQXGLPJUCTOI-WYMLVPIESA-N |
| CID | 9927531 |
| Short Description | Telomerase inhibitor |
References
- E. Pascolo et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J. Biol. Chem. 2002, 277, 15566-15572.
- D.K. Barma et al. Inhibition of telomerase by BIBR 1532 and related analogues. Bioorg. Med. Chem. Lett. 2003, 13, 1333-1336.
- K. Damm et al. A highly selective telomerase inhibitor limiting human cancer cell proliferation. E.M.B.O.J. 2001, 20, 6958-6968.
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