Telomerase Inhibitor

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2.

Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.

BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC₅₀ of 100 nM in a cell-free assay.

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.

Boldine is an aporphine alkaloid telomerase (telomerase) inhibitor (IC₅₀ of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury.

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 is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity.

RHPS4 is a potent telomerase inhibitor (IC₅₀ = 0.33 μM). RHPS4 is a DNA damage inducer.

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).

Imetelstat (GRN163L) is a 13-mer oligonucleotide and competitive Telomerase inhibitor. Imetelstat binds with high affinity to the template region of the RNA component of human telomerase. Imetelstat induces Apoptosis. Imetelstat is capable of selectively eliminating myelofibrosis hematopoietic stem cells. Imetelstat leads to the loss of a cancer cell's ability to maintain telomere length, resulting in the inhibition of cell proliferation.

Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity.

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.

FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research.

Telomerase-IN-3 is a telomerase inhibitor, which directly targets hTERT promoter activity. hTERT is the key component for maintenance of telomerase activity.

TMPyP tetrachloride is a quadruplex-specific ligand. TMPyP tetrachloride inhibits the interaction between G-quadruplexes and IGF-1. TMPyP tetrachloride is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP tetrachloride is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP tetrachloride has antiviral activity against SARS-CoV-2.

L2H2-6OTD diformic is a G-quadruplex (G-quadruplex, G4) ligand and telomerase (telomerase) inhibitor, with an IC₅₀ of 15 nM against human telomerase. L2H2-6OTD diformic induces the formation of antiparallel G-quadruplex structures in long telomeric DNA. L2H2-6OTD diformic stabilizes the G4 structure of GD3 and enhances the immunological activity of CpG ODN. L2H2-6OTD diformic is applicable to research related to the development of G4-CpG immune adjuvants.

β-Rubromycin, a quinone antibacterial agent, is a selective HIV-1 reverse transcriptase inhibitor with a K_i of 0.27 μM. β-Rubromycin is a potent telomerase inhibitor with an IC₅₀ of 3 μM. β-Rubromycin inhibits the proliferation of both K-562 and HeLa cells with IC₅₀ values of 19.5 µM and 22.7 µM, respectively.

Boldine (Standard) is the analytical standard of Boldine (HY-N6973). This product is intended for research and analytical applications. Boldine is an aporphine alkaloid telomerase (telomerase) inhibitor (IC₅₀ of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury.

Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.

Telomerase-IN-1 is a Telomerase inhibitor with an IC₅₀ of 0.19 μM.