- Cat. No.
- A10140
BIBR 1532
BIBR 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).
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Telomerase inhibitors and activators act on telomerase, the reverse transcriptase that extends telomeres. Telomerase activity was first found in 1985 in Tetrahymena extracts, as a terminal transferase that adds telomeric repeats. The human enzyme pairs telomerase reverse transcriptase (TERT) with an RNA template. A 1994 study detected telomerase activity in most immortal cell lines and tumors but rarely in normal somatic tissues. BIBR 1532 inhibits the enzyme directly, while Braco-19, RHPS4 and TMPyP4 tosylate stabilize telomeric G-quadruplex DNA. 6-Thio-dG is a nucleoside that telomerase incorporates into telomeres, and epithalon is listed as an activator. The set also includes the topoisomerase inhibitors amsacrine and GENZ-644282.
BIBR 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).
Costunolide is an Inhibitor of human telomerase activity (IC50 = 65 μM in MCF-7 breast cancer cells). It is described to act as an antioxidant, anti-mycobacterial, anti-inflammatory, and anti-viral, with cytotoxic activity.
Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity.
Braco-19 is a potent telomerase inhibitor that disrupts the capping and catalytic function of telomerase, leading to accelerated cellular senescence or selective cell death. As a G-quadruplex (GQ) binding ligand, Braco-19 effectively stabilizes G-quadruplex formation at the 3' telomeric DNA overhang, enhancing its biological activity. Additionally, Braco-19 demonstrates efficacy as an inhibitor of HAdV virus replication, making it a valuable tool for research in aging, cancer therapeutics, and virology studies.
6-thio-dG is a nucleoside analog and telomerase substrate.
Synonyms: NSC714187
RHPS4 is a potent inhibitor of Telomerase at submicromolar.
Synonyms: TMP 1363
TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
β-Rubromycin is a selective inhibitor of HIV-1 reverse transcriptase, exhibiting a Ki of 0.27 μM. Additionally, it demonstrates potent telomerase inhibition with an IC50 of 3 μM. β-Rubromycin effectively inhibits the proliferation of K-562 and HeLa cell lines, showing IC50 values of 19.5 µM and 22.7 µM, respectively, making it a valuable tool for research in HIV and telomerase-related studies.
Synonyms: GRN163L
Imetelstat is a 13-mer oligonucleotide that functions as a competitive inhibitor of telomerase. By binding with high affinity to the RNA template region of human telomerase, Imetelstat induces apoptosis in cancer cells. This compound selectively eliminates hematopoietic stem cells in myelofibrosis, impairing the ability of cancer cells to maintain telomere length and ultimately inhibiting cell proliferation. Imetelstat's unique mechanism makes it a valuable tool for research applications focused on telomerase activity and cancer therapeutics.
Braco-19 trihydrochloride is a potent telomerase inhibitor that disrupts telomerase capping and catalytic activity. By acting as a G-quadruplex binding ligand, Braco-19 stabilizes G-quadruplex formation at the 3' telomeric DNA overhang, leading to rapid cellular senescence or selective cell death. Additionally, Braco-19 demonstrates efficacy as an inhibitor of HAdV virus replication, making it a valuable tool for research in cancer biology and virology.
L2H2-6OTD is a potent telomerase inhibitor that functions through G-quadruplex stabilization. This compound demonstrates significant telomerase inhibitory activity with an IC50 value of 15 nM, making it a valuable tool in cancer research. It can be utilized to investigate telomere biology, the mechanisms underlying cellular aging, and potential therapeutic strategies targeting telomerase in cancer cells.
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