BIBR 1532
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]
References:
[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.
- 1. Tafseel Hussain, Limin Chai, et al. "Activation of PPAR-γ prevents TERT-mediated pulmonary vascular remodeling in MCT-induced pulmonary hypertension." Heliyon. 2023 Mar 4;9(3):e14173. PMID: 36938425
- 2. Qianqian Zhang, Wei Feng, et al. "PPARγ Agonist Pioglitazone Inhibits PDGF-induced Pulmonary Artery Smooth Muscle Cells Proliferation and Migration via Modulating TERT." Biomed Pharmacother. 2022 Aug;152:113233. PMID: 35689861
- 3. Do?an F, ?zate? 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
- 4. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 331.36 |
| Cas No. | 321674-73-1 |
| Formula | C21H17NO3 |
| Solubility | insoluble in H2O; ≥15.65 mg/mL in DMSO; ≥2.36 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
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Conventional telomerase assay |
For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract was mixed with different concentrations of BIBR 1532 in a final volume of 20 μL. After 15-minute preincubation on ice, 20 μL of the reaction mixture was added, and the reaction was initiated by transferring the tubes to 37 °C. The final concentrations in the reaction mixture were 25 mM Tris-Cl (pH 8.3), 1 mM MgCl2, 1 mM EGTA, 1 mM dATP, 1 mM dTTP, 6.3 μM cold dGTP, 15 μCi [α-32P]dGTP (3000 Ci/mmol), 1.25 mM spermidine, 10 units of RNasin, 5 mM 2-mercaptoethanol, and 2.5 μM TS-primer (5'-AATCCGTCGAGCAGAGTT). |
| Cell experiment [2]: | |
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Cell lines |
Nalm-6 cells |
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Preparation method |
The solubility of this compound in DMSO is > 15.65 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10, 30, 60 and 90 μ M; for 48 hrs |
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Applications |
In Nalm-6 cells, BIBR 1532 at the concentrations of 30, 60 and 90 μM inhibited DNA synthesis rates by 10, 17 and 28%, respectively. MTT assay analysis showed that BIBR 1532 concentration-dependently reduced the metabolic activity of Nalm-6 cells (15, 30 and 44% at the concentrations of 30, 60 and 90 μ M, respectively). At the doses of 10 and 30 μM, BIBR 1532 partially inhibited telomerase activity while at the higher doses, i.e. 60 and 90 μM, BIBR 1532 resulted in marked telomerase inhibition. |
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References: [1]. Pascolo E, Wenz C, Lingner J, Hauel N, Priepke H, Kauffmann I, Garin-Chesa P, Rettig WJ, Damm K, Schnapp A. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [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. |
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| Description | BIBR 1532 is a selective inhibitor of telomerase with IC50 value of 93 nM for human telomerase. | |||||
| Targets | human telomerase | |||||
| IC50 | 93 nM | |||||
Quality Control & MSDS
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Chemical structure
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