BIBR 1532

Catalog No.S1186

BIBR 1532 Chemical Structure

Molecular Weight(MW): 331.36

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 were observed at concentrations vastly exceeding the IC50 for telomerase.

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 110 In stock
USD 470 In stock
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Cited by 4 Publications

2 Customer Reviews

  • (E, F)The cells were not treated or treated with BIBR1532 before wounds were made. Relative ratio of wound closure per field was shown. (G, H) KrasG12D and KrasG12V-induced migration ability of lung cancer cells was inhibited by BIBR1532 in Transwell invasion assay. Numbers of invasive cells in 10 fields were counted. Magnification: ×200. Representative pictures were shown. Values were the mean of 3 determinations ± SEM (one-way ANOVA, *p < 0.05, **p < 0.01).

    Oncotarget, 2017, 8(1):179-190. BIBR 1532 purchased from Selleck.

    J Mol Neurosci 2013 51(1), 187-98. BIBR 1532 purchased from Selleck.

Purity & Quality Control

Choose Selective Telomerase Inhibitors

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 were observed at concentrations vastly exceeding the IC50 for telomerase.
Targets
Telomerase [1]
(Cell-free assay)
100 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells MVXGeY5kfGmxbjDhd5NigQ>? NXXl[41KOiCq NULNS3FwUW6qaXLpeIlwdiCxZjD0[YxwdWW{YYPlJIlvKGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgNkBpenNiYomgX4FteGijLUOyVH1lT1SSIHnuZ49zeG:{YYTpc44h[XO|YYmsJGlEPTB;OUOgcm0> M{f6cFIzPDF|OES1
human MDA-MB-231 cells NUmweGF4TnWwY4Tpc44h[XO|YYm= NXjhSIR[OjRiaB?= MX3Jcohq[mm2aX;uJI9nKHSnbH;t[ZJie2ViaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkAzPCCqcoOgZpkhXFKDUD3QR3IuTUyLU1GsJGlEPTB;MD6xO{DPxE1? NWfNRnhyOjV7NkW3O|g>
human MGC803 cells MlXTSpVv[3Srb36gZZN{[Xl? NIr0[GEzPCCq MlvwTY5pcWKrdHnvckBw\iC2ZXzvcYVz[XOnIHnuJIh2dWGwIF3HR|gxOyClZXzsd{Bi\nSncjCyOEBpenNiYomgWHJCWC2SQ2KtSWxKW0FuIFnDOVA:OC5{ODFOwG0> MorDNlU2PTR7MkK=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[1]

+ Expand

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:

[2]

+ Expand
  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (199.17 mM)
Ethanol 3 mg/mL (9.05 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 331.36
Formula

C21H17NO3

CAS No. 321674-73-1
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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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.

Telomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID