Telomerase

Braco-19 is a telomerase/telomere inhibitor and an inhibitor of HAdV viral replication with antiviral activity that reduces lipid vacuolization in adipocytes, inhibits proliferation and decreases telomerase activity in human glioblastoma cells.

360A is a stabilizing G-Quadruplex ligand, and also inhibits telomerase activity for telomerase in TRAP-G4 assay(IC50 : 300 nM).

Telomerase-IN-1 is a telomerase inhibitor (IC50: 0.19 μM). telomerase-IN-1 activates hTERT expression through the endoplasmic reticulum stress (ERS) of the ER overreaction (EOR), which then induces ERS, leading to apoptosis. telomerase-IN-1 leads to inhibition of cell proliferation through the expression of downstream signaling molecules including Telomease-IN-1 has high inhibitory activity against telomerase, high anti-proliferative capacity against SMMC-7721 cells, and no significant toxic effect on human normal hepatocytes. telomerase-IN-1 in xenograft tumor model exhibited antitumor activity.

The L-778123 hydrochloride is an inhibitor of FPTase (IC50: 2 nM) and GGPTase-I (IC50: 98 nM) in enzyme inhibition determination.

RHPS4 (RHPS 4 methosulfate) is a potent inhibitor of Telomerase at submicromolar.

Zidovudine (ZDV) is a synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zidovudine inhibits DNA polymerase, resulting in the inhibition of DNA replication and cell death. This agent also decreases levels of available pyrimidines.

7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP), a nucleotide analogue, functions as a telomerase inhibitor with an IC50 value of 11 μM [1].

Lipiferolide is an inhibitor of farnesyl protein transferase(FPTase), it inhibits the FPTase activity in a dose-dependent manner, and shows cell growth inhibitory activity against several tumor cells, it possesses cytotoxic activity against KB cells. Liriodenine also has antiplasmodial activity.

BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor (IC50: ~0.2 μM) with anticancer activities. BMVC inhibits Taq DNA polymerase (IC50: ~2.5 μM).

Ceramides Mixture, an endogenous ceramide, consists of hydroxy and non-hydroxy fatty acid-containing ceramides. It is involved in the regulation of cell cycle arrest, growth inhibition, and modulation of telomerase activity.

MST-312 (Telomerase Inhibitor IX) is a derivative of green tea epigallocatechin gallate (EGCG). MST-312 is a telomerase inhibitor. MST-312 has research value in cancer, such as multiple myeloma (MM).

Telomerase-IN-2 (Telomerase inhibitor 2) shows potent inhibitory activity against telomerase by decreasing the expression of dyskerin (IC50: 0.89 µM).

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand and is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.

Braco-19 trihydrochloride (BRACO19 3HCl) is an inhibitor of telomerase and prevents the capping and catalytic action of telomerase. Braco-19 trihydrochloride inhibits HAdV virus replication.

Costunolide (Costus lactone) has anti-inflammatory and anti-oxidant properties and mediates apoptosis.

Cyclogalegenin (Astramembrangenin) is able to elongate telomeres, resulting in increased lifespan of the animals.

BIBR 1532 is an effective, specific and non-competitive telomerase inhibitor (IC50: 100 nM, in a cell-free assay).

360A iodide is a selective stabilizer of G-quadruplex and inhibits telomerase activity (IC50: 300 nM in TRAP-G4 assay).

Astramembrangenin (Cycloastragenol (Astramembrangenin)) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus. Cycloastragenol (CAG) may have a novel therapeutic role in depression

Adefovir is an acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor used for treatment of hepatitis B and herpes simplex virus infection.