G-quadruplex Ligand

Phen-DC3 Trifluoromethanesulfonate is a bisquinolinium G-quadruplex (G4) ligand. Phen-DC3 Trifluoromethanesulfonate selectively binds to and stabilizes the hybrid quadruplex-duplex hybrid (QDH) derived from the PIM1 promoter. Phen-DC3 Trifluoromethanesulfonate also binds to the c-myc promoter Pu24T G4 via extensive π-stacking, and induces polymerase stalling at α-synuclein DNA and RNA G4 sequences. Phen-DC3 Trifluoromethanesulfonate downregulates LPS (HY-D1056)-induced TNFRSF21, RIPK3 and p-MLKL in VECs, and ameliorates CLP-induced pulmonary vascular leakage in septic rats. Phen-DC3 Trifluoromethanesulfonate can be used in studies related to neurodegenerative diseases and sepsis-associated vascular injury.

G-quadruplex ligand 6 is a G-quadruplex ligand targeting the c-MYC promoter with anti-tumor activity. G-quadruplex ligand 6 forms a non-covalent complex with Pu22, a G-quadruplex model of the c-MYC promoter, with a microscopic dissociation constant K_d of 0.202 μM. G-quadruplex ligand 6 selectively inhibits tumor cell proliferation, blocks the binding of transcription factors by stabilizing the G-quadruplex in the c-MYC promoter, and thereby regulates the expression of proto-oncogenes. G-quadruplex ligand 6 can be used in the research of pancreatic cancer, non-small cell lung cancer, colorectal cancer, and triple-negative breast cancer.

SYUIQ-5 is a G-quadruplex ligand. SYUIQ-5 stabilizes G-quadruplex and induce senescence. SYUIQ-5 inhibits c-myc gene promoter activity. SYUIQ-5 induces cancer cells autophagy by triggering telomere damage through TRF2 delocalization from telomeres.

MM41 is a quadruplex-interacting compound. MM41 binds tightly to quadruplexes encoded in the promoter sequences of the BCL-2 and k-RAS genes. MM41 reduces BCL-2 and k-RAS protein levels, increases caspase 3. MM41 has antitumor effects against pancreatic cancer.

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.

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.

MET Transcription-IN-1 (Compound C3) is an orally active MET transcription inhibitor. MET Transcription-IN-1 can efficiently bind and stabilize the G-quadruplex in the MET promoter region, thereby inhibiting c-Met expression. MET Transcription-IN-1 can also overcome drug resistance caused by specific c-Met mutations. MET Transcription-IN-1 is capable of inhibiting tumor cell proliferation, migration, and invasion, as well as inducing cell cycle arrest and apoptosis. MET Transcription-IN-1 has antitumor activity, and can be used in the research of tumors such as non-small cell lung cancer.

BYBC‑1 is a selective G4‑RNA‑targeting ligand with high affinity forKRAS and NRAS G4‑RNAs (K_d = 0.05-0.28 μM). BYBC‑1 stabilizes G4‑RNA structures in KRAS and NRAS mRNA, blocks thePI3K/AKT and MAPK/ERK pathways, activates the DNA damage response (DDR), suppresses energy metabolism, and induces S‑phase arrest and apoptosis. BYBC‑1 exhibits high selectivity over non‑malignant fibroblasts and significantly inhibits the growth of HCT‑116 xenograft tumors in vivo. BYBC‑1 can be used for the study of colorectal cancer.

TOR-G4 is a Fluorescent probe that binds to G-quadruplex (G4) nucleic acid structures. TOR-G4 exhibits a unique fluorescence lifetime when bound to G4 compared to other structures, enabling sensitive discrimination between G4-bound and non-G4-bound states. TOR-G4 mainly colocalizes with RNA in the cytoplasm and nucleolus. TOR-G4 can be used to investigate the roles of RNA G4 in cells. TOR-G4 shows cytotoxicity against osteosarcoma cells.

NOTA-RHAU18 is a conjugate of the chelator NOTA and the peptide RHAU18. NOTA-RHAU18 can be used to synthesize the radiolabeled peptide probe [¹⁸F]AlF-NOTA-RHAU18. [¹⁸F]AlF-NOTA-RHAU18 targets mitochondrial DNA G4. [¹⁸F]AlF-NOTA-RHAU18 can be used to visualize and detect solid tumors in homozygous mice. [¹⁸F]AlF-NOTA-RHAU18 can also be used in PET imaging studies.

Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC₅₀ of 0.4 μM. Telomeric G4s ligand 2 binds to dimeric telomeric G4, inhibits the activities of DHX36 and BLM helicases. Telomeric G4s ligand 2 activates cGAS-STING and TERRA-ZBP1 pathways, inducing autophagy and G2/M cell cycle arrest, and exhibits antiproliferative effects across cancer cell lines. Telomeric G4s ligand 2 can be used for the study of colorectal cancer.

G-quadruplex ligand 5 is a G-quadruplex (G4) ligand. G-quadruplex ligand 5 selectively stabilizes cancer-associated G4 oligonucleotides and shows cytotoxicity toward cancer cells. G-quadruplex ligand 5 can be used for the research of cancer.

G-quadruplex ligand 3 (Compound 16) is a G-quadruplex ligand with anticancer effects that chelate iron. G-quadruplex ligand 3 stabilizes G-quadruplexes in human leukemia Jurkat cells. G-quadruplex ligand 3 localizes in the cell nucleus, serving as a fluorescent nuclear tracer for the labile iron pool.

Phen-DC3 is a bisquinolinium G-quadruplex (G4) ligand. Phen-DC3 selectively binds to and stabilizes the hybrid quadruplex-duplex hybrid (QDH) derived from the PIM1 promoter. Phen-DC3 also binds to the c-myc promoter Pu24T G4 via extensive π-stacking, and induces polymerase stalling at α-synuclein DNA and RNA G4 sequences. Phen-DC3 Trifluoromethanesulfonate (HY-15594A) downregulates LPS (HY-D1056)-induced TNFRSF21, RIPK3 and p-MLKL in VECs, and ameliorates CLP-induced pulmonary vascular leakage in septic rats. Phen-DC3 can be used in studies related to neurodegenerative diseases and sepsis-associated vascular injury.