Home DNA Damage/DNA Repair Telomerase inhibitor - Apoptosis related activator BIBR 1532 For research use only.

BIBR 1532

BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.

BIBR 1532 Chemical Structure

BIBR 1532 Chemical Structure

CAS No. 321674-73-1

Purity & Quality Control

BIBR 1532 Related Products

Signaling Pathway

Telomerase Signaling Pathways

Telomerase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells Function assay 2 h Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay, IC50=93 nM 22413845
human MDA-MB-231 cells Function assay 24 h Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.17 μM 25965778
human MGC803 cells Function assay 24 h Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.28 μM 25554922
HeLa Function assay 15 mins 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, IC50=3.6μM 22413845
HeLa Function assay 15 mins 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, IC50=4.6μM 22413845
HeLa Function assay 30 mins 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, IC50=0.093μM 24053596
HEK293 Function assay Inhibition of human telomerase activity isolated from HEK293 cells assessed as reduction in dNTP incorporation using 5'-biotinylated AATCCGTCGAGCAGAGTT primer by flash plate assay, IC50=3.6μM 27657809
Click to View More Cell Line Experimental Data

Biological Activity

Description BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.
Targets
Telomerase [1]
(Cell-free assay)
100 nM
In vitro
In vitro BIBR 1532 exhibits an non-competitive inhibitory effect on telomerase activity. [1] In JVM13 leukemia cell line, BIBR 1532 shows an antiproliferative effect in a dose-dependent range with IC50 of 52 μM, and similar results are also observed in other leukemia cell lines including Nalm-1, HL-60, and Jurkat. In addition, BIBR 1532 results in a direct antiproliferative effect on acute myeloid leukemia (AML) with IC50 of 56 μM without affecting the proliferative capacity of normal hematopoietic progenitor cells. [2] BIBR 1532 (2.5 μM) reduces colony-forming ability, and induces telomere length shortening as well as chemotherapeutic sensitization by inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/MlnR cell lines. [3] In T-cell prolymphocytic leukemia (T-PLL), BIBR 1532 shows selective cytotoxic effects in a dose-dependent manner and BIBR 1532-treated cells also demonstrates nuclear condensation and formation of apoptotic bodies morphologically compatible with apoptosis. [4] A recent study shows that combination treatment of BIBR 1532 and chemotherapeutic agents carboplatin results in a potential synergy for eliminateing ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines. [5]
Kinase Assay Conventional Telomerase Assay
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
Cell Research Cell lines JVM13
Concentrations 0 to 80 μM
Incubation Time 24 -72 hours
Method

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.

Chemical Information & Solubility

Molecular Weight 331.36 Formula

C21H17NO3
CAS No. 321674-73-1 SDF Download BIBR 1532 SDF
Smiles CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (199.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Does BIBR1532 diffuse through the plasma membrane and nuclear membrane?

Answer:
BIBR1532 is a cell permeable molecule.

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