Telomerase

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.

Amsacrine (m-AMSA) is an anticancer agent that displays activity against refractory acute leukemias as well as Hodgkin's and non-Hodgkin's lymphomas.

Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity.

Epithalon is a synthetic tetra-peptide (Ala-Glu-Asp-Gly),which regulated pineal secretion processes, presumably, via protooncogenes.

6-thio-dG is a nucleoside analog and telomerase substrate.

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.

Astramembrangenin (Cycloastragenol) is a compound isolated from the roots of Astragalus kuhitangi (Nevski) Sirj.

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.

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.

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.