Telomerase Inhibitor

TERT 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.

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.

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.

G-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.

Telomerase-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.

Telomerase-IN-7 (compound 9) is a Telomerase inhibitor with an IC₅₀ of 0.03 μM.

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.

Telomerase-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.

α-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.

Telomerase-IN-6（6f）is a telomerase inhibitor with antitumor activity.

PI3K/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.

TRF2-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.

7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP), a nucleotide analogue, is a telomerase inhibitor (IC₅₀: 11 μM).

FJ-5002 is a telomerase inhibitor with an IC₅₀ of 2 μM. FJ-5002 can induce telomere shortening, increased chromosomal abnormalities, and senescence/crisis-like features in the human leukemia cell line U937. FJ-5002 exhibits antitumor activity and can be used in the study of cancer.

TERT ligand-1 is a PROTAC target protein ligand that can be used to synthesize the PROTAC NU-PRO-1 (HY-174351). NU-PRO-1 induces TERT degradation in cancer cells.

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.

VEGFR-2-IN-69 (Compound 5A) is a dual inhibitor of VEGFR-2 and Telomerase, which upregulates the expression of caspase 3, caspase 8 and caspase 9, while downregulating CDK-2, CDK-4 and CDK-6. VEGFR-2-IN-69 exhibits an IC₅₀ of 15.46 µM against HCT116 cells.

Guanine-2'-deoxy-β-L-ribofuranosyl-5'-O-triphosphate (sodium) is an isomer of dGTP and an inhibitor of telomerase with a K_i of 15 μM for human enzyme.

Abacavir (Standard) is the analytical standard of Abacavir. This product is intended for research and analytical applications. 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.

Diazaphilonic acid is found in the strain of Talaramuces flavus PF1195. Diazaphilonic acid has no antibacterial activity, but inhibits the ability of DNA amplification and telomerase.