BIBR 1532

Catalog No.S1186

For research use only.

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

CAS No. 321674-73-1

Selleck's BIBR 1532 has been cited by 19 publications

Purity & Quality Control

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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

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 MUHGeY5kfGmxbjDhd5NigQ>? M4Lz[FIhcA>? MmnyTY5pcWKrdHnvckBw\iC2ZXzvcYVz[XOnIHnuJIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiMjDodpMh[nliW3HsdIhiNTN{UG3kS3RRKGmwY3;ydI9z[XSrb36gZZN{[XluIFnDOVA:QTNibl2= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjRzM{i0OUc,OjJ2MUO4OFU9N2F-
human MDA-MB-231 cells MY\GeY5kfGmxbjDhd5NigQ>? MYKyOEBp MlzqTY5pcWKrdHnvckBw\iC2ZXzvcYVz[XOnIHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFSUQWCtVGNTNUWOSWPBMEBKSzVyPUCuNVch|ryP NEj4PG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVc4QCd-MkW5OlU4Pzh:L3G+
human MGC803 cells M2fuPWZ2dmO2aX;uJIF{e2G7 MY[yOEBp MUDJcohq[mm2aX;uJI9nKHSnbH;t[ZJie2ViaX6gbJVu[W5iTVfDPFA{KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDUVmFRNVCFUj3FUGlUSSxiSVO1NF0xNjJ6IN88US=> NUDHfmQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVQ6OjJpPkK1OVU1QTJ{PD;hQi=>
HeLa NHfC[HFHfW6ldHnvckBie3OjeR?= Mn;6NVUhdWmwcx?= M1P4NmlvcGmkaYTpc44hd2ZidHXsc41memG|ZTDpckBpfW2jbjDI[WxiKGOnbHzzJJV{cW6pIEWnMWFCXCCFQ1egWGNIKEGJQzDBS2EhT1SWLUOnJIF{KHO3YoP0doF1\SCrbnP1ZoF1\WRiZn;yJFE2KG2rboOgdJJqd3JidH:g[Zh1\W6|aX;uJJJm[WO2aX;uJIJ6KHSnbH;t[ZJq[yC{ZYDlZZQh[W2ybHnmbYNifGmxbjDwdo91d2OxbDygTWM2OD1|LkdOwG0> NUjhNWRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0NVM5PDVpPkKyOFE{QDR3PD;hQi=>
HeLa M3LQd2Z2dmO2aX;uJIF{e2G7 MVexOUBucW6| MYDJcohq[mm2aX;uJI9nKHSnbH;t[ZJie2ViaX6gbJVu[W5iSHXMZUBk\WyuczD1d4lv\yB3Jz3BRXQhS0OJIGTDS{BCT0NiQVfBJGdVXC1|JzDhd{B{fWK|dILheIUhcW6ldXLheIVlKG[xcjCxOUBucW6|IIDybY9zKHSxIHX4eIVve2mxbjDy[YFkfGmxbjDmc4xtd3enZDDifUBkd22yb4Xu[EB4[XOqb4X0JIJ6KHOyaX6teIVtd22ncnnjJJJmeGWjdDDhcZBtcW[rY3H0bY9vKHC{b4TvZ49tNCCLQ{WwQVQvPs7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjRzM{i0OUc,OjJ2MUO4OFU9N2F-
HeLa NGjBS5hHfW6ldHnvckBie3OjeR?= NES3TnM{OCCvaX7z MX7Jcohq[mm2aX;uJI9nKGi3bXHuJJRmdG:vZYLhd4UhcXOxbHH0[YQh\nKxbTDoeY1idiCKZVzhJINmdGy|IH71Z4xm[XJiZYj0doFkfHNiZYjwdoV{e2WmIHnuJIlve2WldDDj[YxteyCjc4Pld5Nm\CCjczDbN|NRZWSFTWCgbY5kd3Kyb4LheIlwdiCjZoTldkA{OCCvaX7zJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTBwMEmz{txO Mn\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUO1PVYoRjJ2MEWzOVk3RC:jPh?=
HEK293 MmHDSpVv[3Srb36gZZN{[Xl? MVPJcohq[mm2aX;uJI9nKGi3bXHuJJRmdG:vZYLhd4Uh[WO2aY\peJkhcXOxbHH0[YQh\nKxbTDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIRPXFBiaX7jc5Jxd3KjdHnvckB2e2mwZzC1K{1jcW:2aX75cIF1\WRiQVHUR2NIXEOJQVfDRWdCT1SWIIDybY1meiCkeTDmcIF{cCCybHH0[UBie3OjeTygTWM2OD1|LkdOwG0> M1K2eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NkW3PFA6Lz5{N{[1O|gxQTxxYU6=

Protocol (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 331.36
Formula

C21H17NO3

CAS No. 321674-73-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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