BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities[1][2].
360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity[1].
Telomerase-IN-3 is a telomerase inhibitor, which directly targets hTERT promoter activity. hTERT is the key component for maintenance of telomerase activity[1].
360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].
Ceramides Mixture is an endogenous ceramide and consists of hydroxy and non-hydroxy fatty acid-containing ceramides. Ceramides Mixture is a main lipid component of the permeability barrier in epidermis. Ceramides Mixture is involved in the regulation of growth inhibition, cell cycle arrest, and modulation of telomerase activity[1][2].
L2H2-6OTD, containing one to four G-quadruplex binding loops, is a telomeric inhibitor analogue. l2H2-6OTD has telomerase inhibitory activity with an IC50 value of 15 nM[1].
MST-312 is a telomerase inhibitor. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 can be used for the research of cancer, such as multiple myeloma (MM)[1].
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research[1].
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].
7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP), a nucleotide analogue, is a telomerase inhibitor (IC50: 11 μM)[1].
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa[1].
Telomerase-IN-1 is a Telomerase inhibitor with an IC50 of 0.19 μM.
TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1[1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines[2].