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BIBR1532

Cat. No. M1676

All AbMole products are for research use only, cannot be used for human consumption.

BIBR1532 Structure
Synonym:

BIBR-1532

Size Price Availability Quantity
10mM*1mL in DMSO USD 49  USD49 In stock
1mg USD 25  USD25 In stock
5mg USD 47  USD47 In stock
10mg USD 80  USD80 In stock
25mg USD 143  USD143 In stock
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Quality Control & Documentation
Biological Activity

BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. 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. The selectivity of BIBR1532 was assessed in a panel of DNA and RNA polymerases, including HIV reverse transcriptase, showing that none of these enzymes  was inhibited at concentrations vastly exceeding the IC50 for telomerase. 

BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity.

Customer Product Validations & Biological Datas
Source Target Oncol (2015). Figure 3. BIBR1532
Method cell apoptosis assay
Cell Lines MCF-7 cells
Concentrations 10 μM
Incubation Time 24 h
Results The drug combination induced 28.67±2.03 % apoptosis, which is significantly higher than apoptosis caused by 20 μM BIBR1532 alone.
Source Target Oncol (2015). Figure 2. BIBR1532
Method colony formation assay
Cell Lines MCF-7 cells
Concentrations 10 μM
Incubation Time 72 h
Results BIBR1532 and paclitaxel alone inhibited cell colony formation in a dose-dependent manner in MCF-7 cells.
Protocol (for reference only)
Cell Experiment
Cell lines JVM13 cells
Preparation method Telomerase activity measurements. Telomerase activity of cell populations was determined using the TeloTaGGG polymerase chain reaction enzyme-linked immunosorbent assay (PCR ELISAPLUS) kit (Roche, Mannheim, Germany) according to the manufacturer’s protocol (telomeric repeat amplification protocol [TRAP] assay). Heat-treated cellular lysates (85°C for 10 minutes) were used as negative controls for each sample. Samples are considered as telomerase positive if the difference in absorbance is higher than 2-fold background activity. WST-1 assays Cells (0.5 to 5*104) were plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) (Roche) was 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 was quantified by ELISA reader after 2, 3, and 4 hours of incubation.
Concentrations 0 ~ 80 μM
Incubation time 24 or 72h
Animal Experiment
Animal models Human MM xenograft murine model in CB 17 SCID-mice
Formulation phosphate-buffered saline (PBS)
Dosages 35 mg/kg daily
Administration intraperitoneally
Chemical Information
Molecular Weight 331.36
Formula C21H17NO3
CAS Number 321674-73-1
Solubility (25°C) DMSO 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Bashash et al. Cancer Invest. Direct short-term cytotoxic effects of BIBR 1532 on acute promyelocytic leukemia cells through induction of p21 coupled with downregulation of c-Myc and hTERT transcription.

[2] Meng et al. Gynecol Oncol. Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells.

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Keywords: BIBR1532, BIBR-1532 supplier, Checkpoint, inhibitors, activators

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