BIBR 1532

• CAT Number: I003146
• CAS Number: 321674-73-1
• Molecular Formula: C21H17NO3
• Molecular Weight: 331.371
• Purity: ≥95%
• Target: Telomerase
• Solubility: DMSO: 66 mg/mL, H2O: <1 mg/mL
• Storage: 3 years -20C powder
• IC50: 100 nM
• IUPAC Name: 2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid
• InChI: InChI=1S/C21H17NO3/c1-14(16-11-10-15-6-2-3-7-17(15)13-16)12-20(23)22-19-9-5-4-8-18(19)21(24)25/h2-13H,1H3,(H,22,23)(H,24,25)/b14-12+
• InChIKey: PGFQXGLPJUCTOI-WYMLVPIESA-N
• SMILES: CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2

BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM.IC50 Value: 100 nMTarget: TelomeraseBIBR 1532 is a selective telomerase inhibitor (IC50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively). Studies indicate that BIBR 1532 inhibits the reverse transcriptase of telomerase, hTERT, and shortens the length of the telomere. In addition, reports indicate that BIBR 1532 has the ability to stop cell proliferation in lung cancer cell studies after 120 days. BIBR 1532 causes telomere shortening in exponentially growing NCI-H460 lung carcinoma cells and eventual growth arrest.

Reference

1:Glucose restriction decreases telomerase activity and enhances its inhibitor response on breast cancer cells: possible extra-telomerase role of BIBR 1532. Wardi L, Alaaeddine N, Raad I, Sarkis R, Serhal R, Khalil C, Hilal G.Cancer Cell Int. 2014 Jul 4;14:60. doi: 10.1186/1475-2867-14-60. eCollection 2014. PMID: 25089119 Free PMC Article2:BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for APL. Bashash D, Ghaffari SH, Zaker F, Kazerani M, Hezave K, Hassani S, Rostami M, Alimoghaddam K, Ghavamzadeh A.Anticancer Agents Med Chem. 2013 Sep;13(7):1115-25. PMID: 23293885 3: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. Bashash D, Ghaffari SH, Zaker F, Hezave K, Kazerani M, Ghavamzadeh A, Alimoghaddam K, Mosavi SA, Gharehbaghian A, Vossough P.Cancer Invest. 2012 Jan;30(1):57-64. doi: 10.3109/07357907.2011.629378. PMID: 22236190 4:Inhibition of telomerase by BIBR 1532 and related analogues. Barma DK, Elayadi A, Falck JR, Corey DR.Bioorg Med Chem Lett. 2003 Apr 7;13(7):1333-6. PMID: 12657276