Telomerase Inhibitor

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.

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 (K_D = 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.

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.

Boldine 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.

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.

PMM-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.

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.