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BIBR 1532 Telomerase inhibitor

Name: BIBR 1532
Brand: Selleck Chemicals
SKU: S1186
Availability: InStock
Rating: 5 (31 reviews)

Cat.No.S1186

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. This compound induces apoptosis in cancer cells.

Chemical Structure

Molecular Weight: 331.36

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Other Telomerase Inhibitors	EGCG ((-)-Epigallocatechin Gallate) Costunolide RHPS 4 methosulfate Cycloastragenol TAC (TERT Activator-1) Cyclogalegenol Braco-19 trihydrochloride L-778123 hydrochloride Epitalon MST-312

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (199.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (30.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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.

Chemical Information, Storage & Stability

Molecular Weight	331.36	Formula	C₂₁H₁₇NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	321674-73-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2

Mechanism of Action

Targets/IC₅₀/Ki	Telomerase (Cell-free assay) 100 nM
In vitro	BIBR 1532 exhibits an non-competitive inhibitory effect on telomerase activity. In JVM13 leukemia cell line, this compound 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, it 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. This chemical (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/Mln^R cell lines. In T-cell prolymphocytic leukemia (T-PLL), it shows selective cytotoxic effects in a dose-dependent manner and this compound-treated cells also demonstrates nuclear condensation and formation of apoptotic bodies morphologically compatible with apoptosis. A recent study shows that combination treatment of this compound and chemotherapeutic agents carboplatin results in a potential synergy for eliminateing ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines.
Kinase Assay	Conventional Telomerase Assay
Kinase Assay	For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract is mixed with different concentrations of BIBR 1532 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
References	[1] https://pubmed.ncbi.nlm.nih.gov/11854300/ [2] https://pubmed.ncbi.nlm.nih.gov/15507522/ [3] https://pubmed.ncbi.nlm.nih.gov/15939802/ [4] https://pubmed.ncbi.nlm.nih.gov/17898784/ [5] https://pubmed.ncbi.nlm.nih.gov/22115853/

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Handling Instructions

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Frequently Asked Questions

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

Answer:
It is a cell permeable molecule.

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