telomerase

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.

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

Telomerase-IN-4 is a potent telomerase inhibitor with antiproliferative properties and apoptosis-inducing effects [1].

Telomerase-IN-3 is an inhibitor of telomerase.

Telomerase-IN-5 is a potent telomerase inhibitor with antiproliferative properties that induces apoptosis [1].

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).

1. Hypericin (Cyclosan) has antineoplastic activity. 2. Hypericin has antibiotic and antiviral activities. 3. Hypericin has antidepressive activity through inhibiting monoamine oxidase enzyme. 4. Hypericin inhibits RANKL-mediated osteoclastogenesis via affecting ERK signalling in vitro and suppresses wear particle-induced osteolysis in vivo.

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.

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.

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

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

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

Epithalon TFA (307297-39-8 free base) (Epithalon TFA) is an anti-aging agent and telomerase activator.

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

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

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

Remodelin hydrobromide (Remodelin HBR) is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.

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

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

Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards therapeutic window of trifluoperazine.Ganoderic acid B has antinociceptive effect

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).

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.

CAUE is a telomerase activity inhibitor in NALM-6 human B-cell leukemia cells.

Telomestatin is an inhibitor of the telomerase, it induces the formation of basket-type G-quadruplex (G4) structures from hybrid-type G-quadruplexes in the telomeric region.

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].

L2H2-6OTD, a telomeric inhibitor analogue characterized by containing one to four G-quadruplex binding loops, exhibits telomerase inhibitory activity with an IC 50 value of 15 nM.

Erucin is a sulforaphane analog found in cruciferous vegtables. Erucin is a telomerase inhibitor. It induces phase II enzyme activity, suppresses cellular proliferation in hepatocellular carcinoma cells, prevents 6-OHDA-induced neurodegenration, and inhib

Macrocalin B is a diterpenoid against tumor cell proliferation and telomerase activity.

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

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

β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990). β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3 References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990).

6-Thio-2'-Deoxyguanosine (β-TGdR) is a nucleoside analog and telomerase substrate.

BMVC4 is a G-quadruplex stabilizer. BMVC4 induces senescence by activation of pathways of response to DNA damage that was independent of its telomerase inhibitory activity.

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.

BCH001 is a specific small-molecule inhibitor of PAPD5.

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

Epithalon (also known as Epitalon or Epithalone) is the synthetic version of the polypeptide Epithalamin which is naturally produced in the pineal gland.