321674-73-1 Usage
Description
BIBR 1532 is a mixed-type non-competitive inhibitor of telomerase (IC50 = 93 nM) that has little effect on several mammalian DNA and RNA polymerases, bacterial DNA helicase, or HIV-1 reverse transcriptase. It specifically targets the telomerase reverse transcriptase catalytic subunit, TERT. Through its effects on telomerase, BIBR 1532 induces senescence or apoptosis in cancer cells. Apoptosis in triple negative breast cancer cells induced by BIBR 1532 is potentiated by glucose restriction.
Uses
BIBR 1532 is a mixed-type non-competitive inhibitor of telomerase. It specifically targets the telomerase reverse transcriptase catalytic subunit, TERT.
Biological Activity
Selective telomerase inhibitor (IC 50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively). Causes telomere shortening in exponentially growing NCI-H460 lung carcinoma cells and eventual growth arrest.
references
[1]. damm, k.; hemmann, u.; garin-chesa, p.; hauel, n.; kauffman, i.; priepke, h.; niestroj, c.; daiber, c.; enenkel, b.; guilliard, b.; lauritsch, i.; muller, e.; pascolo, e.; sauter, g.; pantic, m.; martens, u. m.; wenz, c.; linger, j.; kraut, n.; rettig, w. j.;schnapp, a. a highly selective telomerase inhibitor limiting human cancer cell proliferation. embo j. 2001, 20, 6958?6968.[2]. bashash d1, ghaffari sh, mirzaee r, alimoghaddam k, ghavamzadeh a. telomerase inhibition by non-nucleosidic compound bibr1532 causes rapid cell death in pre-b acute lymphoblastic leukemia cells. leuk lymphoma. 2013 mar;54[4]:561-8. doi: 10.3109/10428194.2012.704034. epub 2012 sep 28.[3]. bashash d1, 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. bibr 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for apl.
Check Digit Verification of cas no
The CAS Registry Mumber 321674-73-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,2,1,6,7 and 4 respectively; the second part has 2 digits, 7 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 321674-73:
(8*3)+(7*2)+(6*1)+(5*6)+(4*7)+(3*4)+(2*7)+(1*3)=131
131 % 10 = 1
So 321674-73-1 is a valid CAS Registry Number.
InChI:InChI=1/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+
321674-73-1Relevant articles and documents
TELOMERASE REVERSE TRANSCRIPTASE DEGRADERS AND METHODS OF USE THEREOF
-
, (2020/12/30)
The present disclosure provides TERT inhibitor compounds, a TERT inhibitor linked to a ubiquitin ligase ligand, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of inhibiting telomerase reverse transcriptase (TERT) and methods of treating or preventing a disease or disorder using said compounds and/or compositions.
Inhibition of telomerase by BIBR 1532 and related analogues
Barma,Elayadi, Anissa,Falck,Corey, David R.
, p. 1333 - 1336 (2007/10/03)
BIBR 1532 has been reported to be a potent, small molecule inhibitor of human telomerase, suggesting it as a lead for the development of anti-telomerase therapy. We confirm the ability of BIBR 1532 to inhibit telomerase and report the discovery of an equa
