Telomerase
Telomerase is a DNA polymerase that extends the 3' ends of chromosomes by processively synthesizing multiple telomeric repeats. It is a unique ribonucleoprotein (RNP) containing a specialized telomerase reverse transcriptase (TERT) and telomerase RNA (TER) with its own template and other elements required with TERT for activity (catalytic core), as well as species-specific TER-binding proteins important for biogenesis and assembly (core RNP); other proteins bind telomerase transiently or constitutively to allow association of telomerase and other proteins with telomere ends for regulation of DNA synthesis.
Telomerase activity is responsible for the maintenance of chromosome end structures (telomeres) and cancer cell immortality in most human malignancies, making telomerase an attractive therapeutic target. Indeed, a telomerase inhibitor is expected to provide a therapeutic benefit in most cancers while having little side-effects. The adult stem cells that express telomerase in normal tissues divide slowly and have long telomeres, therefore they should be less impacted by telomerase inhibition than the cancer cells which divide rapidly and usually possess short telomeres.
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Telomerase Related Products (57)
Related Products (57)
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Boldine (Standard)
0 ImagesBoldine (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.
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Hypericin (Standard)
0 ImagesHypericin (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.
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Telomerase-IN-1
0 ImagesTelomerase-IN-1 is a Telomerase inhibitor with an IC50 of 0.19 μM.
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TelN Protelomerase
0 ImagesCat. No.: HY-E70576CAS No.: 2747966-35-2TelN Protelomerase is a prokaryotic telomerase of bacteriophage N15. TelN Protelomerase is an enzyme with cleaving-joining activity, which is required for the formation of linear prophage DNA with closed ends in lysogenic bacteria. TelN Protelomerase cleaves both DNA strands and joins the resulting ends to form covalently closed hairpin structures.
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Telomerase-IN-2
0 ImagesTelomerase-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.
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TRF1-TIN2 PPI-IN-1
0 ImagesCat. No.: HY-172662Purity: 99.85%TRF1-TIN2 PPI-IN-1 (Compound 40) is a TRF1-TIN2 interaction inhibitor. TRF1-TIN2 PPI-IN-1 binds to the TRFH domain of TRF1 (KD = 29 μM) and competitively inhibits the binding of the TIN2 peptide (IC50 = 67 μM). TRF1-TIN2 PPI-IN-1 disrupts the interaction between TRF1 and TIN2 by occupying the hotspot region of the TRF1-TIN2 binding interface. TRF1-TIN2 PPI-IN-1 can expel TRF 1 from the shelterin complex and can be used to study shelterin-related cancers.
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TERT activator-2
0 ImagesTERT activator-2 (Compound 1030) is a telomerase reverse transcriptase (TERT) activator that can increase the expression of TERT in cells. TERT activator-2 can be used in telomere-related cell lifespan research.
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Abacavir hydrochloride
0 ImagesCat. No.: HY-17423ECAS No.: 136777-48-5Abacavir 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.
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Abacavir monosulfate
0 ImagesAbacavir 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.
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Boldine hydrochloride
0 ImagesCat. No.: HY-W683756CAS No.: 16625-69-7Boldine hydrochloride 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 hydrochloride 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 hydrochloride blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine hydrochloride exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine hydrochloride can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury.
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G-quadruplex ligand 4
0 ImagesCat. No.: HY-179480G-quadruplex ligand 4 is a chromenone derivative and is a human telomerase reverse transcriptase (hTERT) G4 ligand. G-quadruplex ligand 4 downregulates hTERT expression and exhibits notable cytotoxicity towards triple-negative breast cancer (TNBC) cell lines. G-quadruplex ligand 4 can cause S/G2 cell cycle arrest and induce apoptosis. G-quadruplex ligand 4 downregulates the expression of hTERT, KRAS, and BCL-2. G-quadruplex ligand 4 can be used for the research of TNBC.
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Telomerase-IN-8
0 ImagesCat. No.: HY-204056CAS No.: 1884341-01-8Telomerase-IN-8 is an orally active telomerase inhibitor, with an IC50 value of 0.98 μM. Telomerase-IN-8 exhibits potent antiproliferative activity against multiple tumor cell lines, including PC3, Bcap-37, MGC-803 and HepG2. Telomerase-IN-8 demonstrates potent antitumor efficacy in S180 sarcoma or HepG2 hepatoma xenograft mice. Telomerase-IN-8 can be used for the study of telomerase-targeted anticancer.
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Telomerase-IN-7
0 ImagesCat. No.: HY-163914CAS No.: 444320-44-9Telomerase-IN-7 (compound 9) is a Telomerase inhibitor with an IC50 of 0.03 μM.
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Abacavir sulfate (Standard)
0 ImagesSynonyms: Abacavir Hemisulfate (Standard); ABC sulfate (Standard)Abacavir (sulfate) (Standard) is the analytical standard of Abacavir (sulfate). This product is intended for research and analytical applications. 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.
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PMM-302
0 ImagesCat. No.: HY-186330CAS No.: 2763421-81-2Synonyms: PMMB-302PMM-302 (PMMB-302) is a shikonin N-benzyl sophoridate derivative and a telomerase inhibitor. PMM-302 downregulates the telomerase core proteins DKC1 and NHP2 as well as TERT mRNA, and inhibits telomerase activity. PMM-302 induces G2/M phase cell cycle arrest and apoptosis, accompanied by downregulation of Bcl2, Bcl-XL, and FADD and upregulation of cleaved caspase-3 and cleaved caspase-9. PMM-302 can be used for lung cancer-related research.
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Telomerase-IN-9
0 ImagesCat. No.: HY-179391Telomerase-IN-9 is a potent and selective telomerase inhibitor. Telomerase-IN-9 significantly reduces telomerase activity by binding to hTERT, leading to decreased telomerase function. Telomerase-IN-9 induces apoptosis and inhibits colony formation. Telomerase-IN-9 reduces tumor burden, restores antioxidantbalance, and preserves lung architecture in a Benzo[a]pyrene (HY-107377)-induced lung cancer mouse model. Telomerase-IN-9 can be used for the research of lung cancer.
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α-Rubromycin
0 ImagesCat. No.: HY-119787CAS No.: 27267-69-2Synonyms: Collinomycinα-Rubromycin (Collinomycin) is an antibiotic isolated from the mycelia of Streptomyces collinus. α-Rubromycin also acts as a DNA polymerase inhibitor, with an IC50 of 0.91 μM against bovine mammalian DNA polymerase. α-Rubromycin binds to the active region of DNA polymerase β, competes with nucleotide substrates for binding, and interferes with template-DNA interactions. α-Rubromycin inhibits the activities of telomerase, retroviral reverse transcriptase and terminal deoxynucleotidyl transferase, as well as the growth of Staphylococcus aureus. α-Rubromycin can be used in studies related to bacterial infections.
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Telomerase-IN-6
0 ImagesCat. No.: HY-163137CAS No.: 3032480-07-9Telomerase-IN-6（6f）is a telomerase inhibitor with antitumor activity.
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PI3K/mTOR-IN-19
0 ImagesCat. No.: HY-179155PI3K/mTOR-IN-19 is an orally active, potent, selective PI3K (IC50 = 4.23 nM) and mTOR (IC50 = 2.3 nM) inhibitor. PI3K/mTOR-IN-19 significantly inhibits Eca109 cell viability and induces apoptosis. PI3K/mTOR-IN-19 causes G0/G1 cell cycle arrest, decreased mitochondrial membrane potential, and demonstrates marked telomerase inhibitory activity. PI3K/mTOR-IN-19 modulates the expression of key apoptotic regulators (Bcl-2, Bax, and p53) and downregulates the PI3K/Akt/mTOR signaling pathway. PI3K/mTOR-IN-19 can be used for the study of esophageal cancer.
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TRF2-IN-1
0 ImagesTRF2-IN-1 (compound F2) is a potent telomere repeat-binding factor 2 (TRF2) inhibitor. TRF2-IN-1 shows antiproliferative activity. TRF2-IN-1 induces apoptosis. TRF2-IN-1 directly bind to the TRF2TRFH domain and selectively inhibits TRF2 protein expression and telomeric localization. TRF2-IN-1 shows anticancer activity. TRF2-IN-1 has the potential for the research of osteosarcoma.
