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BIBR 1532

In stock
Catalog No.
A1945
Telomerase inhibitor,novel and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$99.00
In stock
5mg
$50.00
In stock
25mg
$150.00
In stock
100mg
$400.00
In stock

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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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt331.36
Cas No.321674-73-1
FormulaC21H17NO3
Solubility≥15.65mg/mL in DMSO
Chemical Name2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid
SDFDownload SDF
Canonical SMILESCC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Kinase experiment [1]:

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]:

Cell lines

Nalm-6 cells

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.

Reacting condition

10, 30, 60 and 90 μ M; for 48 hrs

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.

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.

Biological Activity

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

Chemical structure

BIBR 1532

Related Biological Data

BIBR 1532

Related Biological Data

BIBR 1532