g-quadruplex

Pyridostatin (RR82) is a synthetic small-molecule stabilizer of G-quadruplexes, a secondary structure of DNA that usually exists in the end of the chromosome or the telomeres.

BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor (IC50: ~0.2 μM) with anticancer activities, and it also inhibits Taq DNA polymerase (IC50: ~2.5 μM).

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand and telomerase inhibitor that exhibits antitumor effects in osteosarcoma cell lines.

BMVC-8C3O is a DNA G-quadruplex (G4) ligand that induces a topological conversion from a nonparallel to parallel form in human telomeric DNA G4.

BMVC2 (o-BMVC), a carbazole derivative of BMVC, is a G-quadruplex (G4) stabilizer.

Pyridostatin Trihydrochloride (RR-82 Trihydrochloride) is a G-quadruplexe stabilizer, with a Kd of 490 nM.

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2.

MM41 is a human telomeric and gene promoter DNA quadruplex stabilizer with an IC50 of <10 nM against the MIA PaCa-2 pancreatic cancer cell line.

360A is a stabilizing G-Quadruplex ligand, and also inhibits telomerase activity for telomerase in TRAP-G4 assay(IC50 : 300 nM).

G-quadruplexligand 3 (Compound 16) is a G-quadruplex ligand with the ability to chelate iron and exhibits anticancer properties. It stabilizes G-quadruplex structures within human leukemia Jurkat cells. Additionally, G-quadruplexligand 3 is localized in the cell nucleus and serves as a fluorescent nuclear tracer for the labile iron pool.

G-quadruplex ligand 2 (compound A3) is a triphenylamine-based ligand that targets mitochondrial DNA G4. It activates the cGAS-STING pathway and inhibits tumor growth and metastasis by regulating the tumor microenvironment (TME).

Compound E1, also known as G-quadruplex DNA fluorescence probe 1, is a selective fluorescent probe targeting G-quadruplex DNA. It possesses the ability to penetrate membranes and enter living cells, demonstrating low cytotoxicity [1].

Carboxy-pyridostatin, as a fluorescent probe, can target G-quadruplex structures and trap cytoplasmic RNA G-quadruplex structures in cells.

APTO-253 (LOR-253) inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through the induction of the KLF4 tumor suppressor.

360A iodide is a selective G-quadruplex stabilizer that inhibits telomerase activity (IC50: 300 nM in TRAP-G4 assay).

Phen-DC3 is a G-quadruplex (G4) specific ligand that inhibits FANCJ and DinG helicases with IC50 values of 65±6 nM and 50±10 nM, respectively.

Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand that inhibits FANCJ and DinG helicases with IC50s of 65±6 nM and 50±10 nM, respectively.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA template.

SJ26 is a Wnt1 inhibitor known for its anticancer activity. It inhibits the expression of WNT1 and the downstream signaling pathways mediated by WNT1 in a G-quadruplex structure-dependent manner, thereby suppressing the migratory activity of cancer cells.

Anticanceragent 263 (compound 7) is an effective anticancer agent. It binds with the G-quadruplex DNA (G4) sequence 22-mer Pu22 (a c-Myc DNA analog). As a structural modulator, Anticanceragent 263 significantly enhances the formation of protein α-helices and has the capacity to form a supramolecular network. Furthermore, Anticanceragent 263 exhibits no cytotoxicity.

SYUIQ-5 is a ligand for G-quadruplex structures. It plays a role in stabilizing G-quadruplexes and inducing senescence. Additionally, SYUIQ-5 inhibits the activity of the c-myc gene promoter. By displacing TRF2 from telomeres, SYUIQ-5 induces telomeric damage, which triggers autophagy (autophagy) in cancer cells.

RNA binder 1 (Compound 4b) is an RNA-binding agent capable of crossing the blood-brain barrier. It selectively binds to the G-quadruplex structure of the G4C2 repeat sequence RNA of the C9orf72 gene. This compound significantly reduces levels of the toxic polypeptides poly(GA) and poly(GP) in cells derived from amyotrophic lateral sclerosis (ALS) patients, while it has no significant impact on the antisense polypeptide poly(PR), demonstrating selectivity for sense RNA. RNA binder 1 is useful for studying ALS and frontotemporal dementia (FTD).

Telomeric G4s ligand 1 is a telomere G-quadruplex ligand that stabilizes telomeric G4 structures and induces the formation of R-loops, leading to DNA damage responses. It prompts apoptosis in tumor cells and triggers immunogenic cell death (ICD).

Anticanceragent 239 (Compound 5) is a ligand for the hTERT promoter G-quadruplex DNA structure (hTERT G4) with a dissociation constant (Kd) of 1.1 μM and reduces hTERT expression. It decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Additionally, Anticanceragent 239 causes mitochondrial dysfunction, disrupts iron metabolism, and activates ferroptosis in cancer cells. It also inhibits tumor growth in MDA-MB-231 xenograft mouse models.