BIBR 1532
Based on 8 publication(s) in Google Scholar
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
The BIBR 1532 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Reinheit: 99.76%
- CAS. Nr.: 321674-73-1
- Formel: C21H17NO3
- Molecular Weight:331.36
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) BIBR 1532
More- Int J Oncol. 2022 Nov;61(5):139. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
- PLoS One. 2024 Oct 25;19(10):e0312115. [Abstract]
- Research Square Preprint. 2025 Jan 05.
- bioRxiv. 2024 August 07.
- Research Square Preprint. 2021 Apr.
- Patent. US20180263995A1.
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Cell Imaging/Staining
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Cell Imaging/Staining
Biologische Aktivität
IC50: 100 nM (telomerase)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.73 μM
Compound: BIBR1532
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Antiproliferative activity against human A549 cells by CCK8 assay
Antiproliferative activity against human A549 cells by CCK8 assay
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[PMID: 34922028] |
| Calu-3 | IC50 |
0.21 μM
Compound: BIBR1532
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Antiproliferative activity against human Calu-3 cells by CCK8 assay
Antiproliferative activity against human Calu-3 cells by CCK8 assay
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[PMID: 34922028] |
| CT26 | IC50 |
42.905 μM
Compound: BIBR1532
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Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
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[PMID: 39140071] |
| GES1 | IC50 |
205.811 μM
Compound: BIBR1532
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Cytotoxicity against human GES1 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Cytotoxicity against human GES1 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
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[PMID: 39140071] |
| HeLa | IC50 |
0.012 μM
Compound: BIBR1532
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Antiproliferative activity against human HeLa cells by CCK8 assay
Antiproliferative activity against human HeLa cells by CCK8 assay
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[PMID: 34922028] |
| HeLa | IC50 |
0.093 μM
Compound: 13, BIBR1532
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Inhibition of human telomerase isolated from human HeLa cells nuclear extracts expressed in insect cells assessed as [33P]dCMP incorporation after 30 mins by liquid scintillation counting analysis
Inhibition of human telomerase isolated from human HeLa cells nuclear extracts expressed in insect cells assessed as [33P]dCMP incorporation after 30 mins by liquid scintillation counting analysis
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[PMID: 24053596] |
| HeLa | IC50 |
0.093 μM
Compound: 2, BIBR-1532
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Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay
Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay
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[PMID: 22413845] |
| HeLa | IC50 |
3.6 μM
Compound: 2, BIBR-1532
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Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
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[PMID: 22413845] |
| HeLa | IC50 |
4.6 μM
Compound: 2, BIBR-1532
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Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol
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[PMID: 22413845] |
| HL-60 | IC50 |
47.824 μM
Compound: BIBR1532
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Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay
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[PMID: 39140071] |
| L02 | IC50 |
80.45 μM
Compound: BIBR1532
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Cytotoxicity against human L02 cells by CCK8 assay
Cytotoxicity against human L02 cells by CCK8 assay
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[PMID: 34922028] |
| MCF7 | IC50 |
0.52 μM
Compound: BIBR1532
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Antiproliferative activity against human MCF7 cells by CCK8 assay
Antiproliferative activity against human MCF7 cells by CCK8 assay
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[PMID: 34922028] |
| MDA-MB-231 | IC50 |
0.17 μM
Compound: BIBR1532
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Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA
Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA
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[PMID: 25965778] |
| MDA-MB-231 | IC50 |
0.17 μM
Compound: BIBR1532
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Antiproliferative activity against human MDA-MB-231 cells by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells by CCK8 assay
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[PMID: 34922028] |
| MGC-803 | IC50 |
0.28 μM
Compound: BIBR1532
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Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA
Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA
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[PMID: 24119869] |
| MGC-803 | IC50 |
0.28 μM
Compound: BIBR1532
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Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA
Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA
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[PMID: 25554922] |
| MGC-803 | IC50 |
0.41 μM
Compound: BIBR1532
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Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA
Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA
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[PMID: 25812966] |
| NCI-H1650 | IC50 |
0.52 μM
Compound: BIBR1532
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Antiproliferative activity against human H1650 cells by CCK8 assay
Antiproliferative activity against human H1650 cells by CCK8 assay
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[PMID: 34922028] |
| NCI-H460 | IC50 |
0.39 μM
Compound: BIBR1532
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Antiproliferative activity against human H460 cells by CCK8 assay
Antiproliferative activity against human H460 cells by CCK8 assay
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[PMID: 34922028] |
BIBR 1532 non-competitively inhibits telomerase activity[1]. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR 1532 exerts antiproliferative effect on acute myeloid leukemia (AML) with IC50 of 56 μM with no effect on the proliferative capacity of normal hematopoietic progenitor cells[2]. BIBR 1532 (2.5 μM) reduces colony-forming ability, induces telomere length shortening and causes chemotherapeutic sensitization via inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/MlnR cell lines[3]. BIBR 1532 is cytotoxic in a dose-dependent manner in T-cell prolymphocytic leukemia (T-PLL)[4]. BIBR 1532 in combination with carboplatin (a chemotherapeutic agent) eliminates ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 321674-73-1
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Appearance Solid
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Molecular Weight 331.36
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Formel C21H17NO3
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Color White to light yellow
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SMILES
O=C(O)C1=CC=CC=C1NC(/C=C(C2=CC=C3C=CC=CC3=C2)\C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Int J Oncol
2022 Nov;61(5):139. PMID: 36169178
BIBR 1532 purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2022 Nov;61(5):139. [Abstract]
BIBR 1532 (0.1, 1, 5, 10, 20, 40, 80, 160 and 320 µM; 5 days) inhibited cell proliferation in a dose-dependent manner in GWH04, U87 and GL15 cells.
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J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
J Cell Physiol
Telomere Attrition-Induced Senescence in Human Pluripotent Stem Cell-Derived Astrocytes: Distinct Cellular and Functional Characteristics. [Abstract]2025 Dec;240(12):e70118. PMID: 41340457
BIBR 1532 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
Representative immunofluorescence images of NPCs stained with NESTIN and SOX1 treated with various concentration of BIBR 1532 (BIBR; 0, 10 , 20 , 40 μM; 10 days).
BIBR 1532 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
A growth curve of NPCs differentiating from hPSCs, treated with BIBR 1532 (BIBR) at concentration of 0, 10, and 20μM. Cell viability was monitored from the initiation of differentiation (day 0) to day 14.
BIBR 1532 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
BIBR 1532 (BIBR; 10 μM; 16 days) did not affect astrocyte differentiation efficiency. In boththe vehicle‐treated control and BIBR‐treated groups, over 90% cell were positive for all tested markers, with no statistically significantdifference between the groups
BIBR 1532 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
BIBR 1532 (BIBR; 10 μM; 16 days) had significantlylarge and flattened cell bodies, with highly branched and elongatedprocesses and often multiple nuclei, a phenom-enon referred to as multinucleation.
BIBR 1532 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
BIBR 1532 (BIBR; 10 μM; 16 days) showed an increased proportion ofsenescence‐associated β‐galactosidase‐positive cells compared to the vehicle‐treated astrocyte culture.
BIBR 1532 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2025 Dec;240(12):e70118. [Abstract]
BIBR 1532 (BIBR; 10 μM; 16 days) revealed significantly more BODIPY‐positive cells. Representative images of LDs (BODIPY 493/503, green) in astrocytes, withcytoplasm defined by Phalloidin‐labeled actin filaments (red).
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PLoS One
The mechanism of NF-κB-TERT feedback regulation of granulosa cell apoptosis in PCOS rats. [Abstract]2024 Oct 25;19(10):e0312115. PMID: 39453929 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (301.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract is mixed with different concentrations of BIBR1532 in a final volume of 20 μL. After 15-minute preincubation on ice, 20 μL of the reaction mixture is added, and the reaction is initiated by transferring the tubes to 37°C. The final concentrations in the reaction mixture are 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; NEN), 1.25 mM spermidine, 10 units of RNasin, 5 mM 2-mercaptoethanol, and 2.5 μM TS-primer (5'-AATCCGTCGAGCAGAGTT). For the recombinant enzyme, 1-7 μL of affinity-purified telomerase (containing less than 0.025 μM hTERT) are assayed in a final volume of 40 μL containing 50 mM Tris acetate (pH 8.5), 50 mM KCl, 1 mM MgCl2, 1 mM spermidine, 5 mM 2-mercaptoethanol, 1 mM dATP, 1 mM dTTP, 2.5 μM dGTP, 15 μCi of [α-32P]dGTP (3000 Ci/mmol) and 2.5 μM (TTAGGG)3. The reaction is initiated by incubation at 37°C for 2 hours and stopped by addition of 50 μL of RNase mix (0.1 mg/mL RNaseA-100 u/mL RNaseT1 in 10 mM Tris-Cl (pH 8.3) and 20 mm EDTA) and incubation for 20 min at 37°C. Samples are deproteinated by adding 50 μL of 0.3 mg/m proteinase K in 10 mM Tris-Cl (pH 8.3) and 0.5% w/v SDS, for a 30-minute incubation at 37°C. DNA is recovered by phenol extraction and ethanol precipitation, and the extension products are analyzed on an 8% (endogenous telomerase) or 12% (recombinant telomerase) polyacrylamide-urea gel. Dried gels are exposed to a Kodak phosphorimager screen, and the results are analyzed.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells are plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) is added, which is transformed into formazan by mitochondrial reductase systems. The increase in the number of viable cells results in an increase of activity of mitochondrial dehydrogenases, leading to an increase of formazan dye formed, which is quantified by ELISA reader after 2, 3, and 4 hours of incubation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Pascolo E, et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [Content Brief]
[2]. El-Daly H, et al. Selective cytotoxicity and telomere damage in leukemia cells using the telomerase inhibitor BIBR1532. Blood. 2005 Feb 15;105(4):1742-9. [Content Brief]
[3]. Ward RJ, et al. Pharmacological telomerase inhibition can sensitize drug-resistant and drug-sensitive cells to chemotherapeutic treatment. Mol Pharmacol. 2005 Sep;68(3):779-86. [Content Brief]
[4]. A Röth, et al. Short telomeres and high telomerase activity in T-cell prolymphocytic leukemia. Leukemia. 2007 Dec;21(12):2456-62. [Content Brief]
[5]. Meng E, et al. Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells. Gynecol Oncol. 2012 Mar;124(3):598-605. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0179 mL | 15.0893 mL | 30.1787 mL | 75.4466 mL |
| 5 mM | 0.6036 mL | 3.0179 mL | 6.0357 mL | 15.0893 mL | |
| 10 mM | 0.3018 mL | 1.5089 mL | 3.0179 mL | 7.5447 mL | |
| 15 mM | 0.2012 mL | 1.0060 mL | 2.0119 mL | 5.0298 mL | |
| 20 mM | 0.1509 mL | 0.7545 mL | 1.5089 mL | 3.7723 mL | |
| 25 mM | 0.1207 mL | 0.6036 mL | 1.2071 mL | 3.0179 mL | |
| 30 mM | 0.1006 mL | 0.5030 mL | 1.0060 mL | 2.5149 mL | |
| 40 mM | 0.0754 mL | 0.3772 mL | 0.7545 mL | 1.8862 mL | |
| 50 mM | 0.0604 mL | 0.3018 mL | 0.6036 mL | 1.5089 mL | |
| 60 mM | 0.0503 mL | 0.2515 mL | 0.5030 mL | 1.2574 mL | |
| 80 mM | 0.0377 mL | 0.1886 mL | 0.3772 mL | 0.9431 mL | |
| 100 mM | 0.0302 mL | 0.1509 mL | 0.3018 mL | 0.7545 mL |