Telomerase

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

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).

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

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.

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.

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

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

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.

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

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

Abacavir (Ziagen) is a nucleoside reverse transcriptase inhibitor analog of guanosine. This agent decreases HIV viral loads, retards or prevents the damage to the immune system, and reduces the risk of developing AIDS.

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

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

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

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.

Abacavir sulfate (Ziagen) , a nucleoside analogue, effectively utilize its antiviral activity

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

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

Antipsychotic agent 54 is a benzoylpiperidine compound that can be used in the study of central nervous system diseases such as psychosis and cognitive impairment.

TAC (TERT activator compound) is a TERT (telomerase reverse transcriptase) activator that enhances TERT transcriptional activity through the MEK/ERK/AP-1 cascade pathway, promotes telomere synthesis in primary human cells and naturally aged mice, reduces cellular senescence and inflammatory cytokines, and alleviates neuroinflammation, among other effects.

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

Tertomotide (GV1001) hydrochloride is a peptide vaccine composed of a 16-amino acid sequence from human telomerase reverse transcriptase (hTERT). It exhibits neuroprotective properties and has potential for research in Alzheimer's disease.

TRF1-TIN2 interaction-IN-1 (Compound 40) is an inhibitor of the TRF1-TIN2 interaction. It binds to the TRFH domain of TRF1 (KD= 29 μM) and competitively inhibits the binding of the TIN2 peptide (IC50= 67 μM). By occupying a hotspot at the TRF1-TIN2 interface, TRF1-TIN2 interaction-IN-1 disrupts the interaction between TRF1 and TIN2. This compound can remove TRF1 from the shelterin complex, making it useful for research on shelterin-related cancers.

Abacavir monosulfate is an orally active, competitive nucleoside reverse transcriptase inhibitor that effectively inhibits HIV replication. Additionally, it exhibits anticancer properties in prostate cancer cell lines, and has the ability to penetrate the blood-brain-barrier and suppress telomerase activity [1] [2] [3].