telomere

BCH001 is a specific small-molecule inhibitor of PAPD5.

FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanisms in hepatocellular carcinoma cells. This leads to T-loop defects, inducing telomere shortening and cellular senescence. Additionally, FKB04 inhibits tumor growth in a human liver cancer xenograft mouse model (by implanting Huh-7 cells in BALB/c mice). This compound is utilized in research focused on liver cancer.

TAC (TERT activator compound) is a TERT (telomerase reverse transcriptase) activator that enhances TERT transcriptional activity through the MEK/ERK/AP-1 cascade pathway, promotes telomere synthesis in primary human cells and naturally aged mice, reduces cellular senescence and inflammatory cytokines, and alleviates neuroinflammation, among other effects.

TRF2-IN-1 (compound F2) is a potent inhibitor of telomere repeat-binding factor 2 (TRF2). It exhibits antiproliferative activity and induces apoptosis. TRF2-IN-1 binds directly to the TRF2TRFH domain, selectively inhibiting TRF2 protein expression and telomere localization. Additionally, TRF2-IN-1 possesses anticancer properties and shows potential for osteosarcoma research.

TERT activator-2 (Compound 1030) is an activator of telomerase reverse transcriptase (TERT), which enhances the expression levels of TERT within cells. TERT activator-2 is applicable to research related to cellular lifespan and telomere functions.

L2H2-6OTDintermediate-3 is an intermediate compound used in the synthesis of L2H2-6OTD, which is applicable in ADC preparation. L2H2-6OTD is a telomere inhibitor analogue with telomerase inhibitory activity (IC50: 15 nM).

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.

Braco-19 is a telomerase/telomere inhibitor and an inhibitor of HAdV viral replication with antiviral activity that reduces lipid vacuolization in adipocytes, inhibits proliferation and decreases telomerase activity in human glioblastoma cells.

Dot1L-IN-7 (compound 25) is a selective and potent inhibitor of telomere silencing 1-like protein (DOT1L) with an IC50 of 1.0 μM. It selectively kills MLL-AF9 cells without affecting the growth of E2A-HLF cells.

ETP-47037 is a potent inhibitor of the PI3Kα isoform (IC50: 0.99 nM) and inhibits the PI3Kβ (IC50: 49.2 nM), PI3Kδ (IC50: 7.13 nM) and PI3Kγ (IC50: 49.1 nM) isoforms. ETP-47037 has potential for telomere protection chemoregulation studies.

CRT0063465 is a ligand for both human Phosphoglycerate Kinase 1 (PGK1) and the stress sensor protein DJ-1, exhibiting a dissociation constant (Kd) of 24 μM for PGK1. Additionally, it influences the composition of the shelterin complex and modulates telomere length [1].

1-PP-myo-InsP5 is a type of inositol pyrophosphate. In mammals, it functions as a signaling molecule by interacting with specific receptors or through non-enzymatic phosphate transfer. Additionally, 1-PP-myo-InsP5 is involved in various biological processes, such as insulin signaling and the regulation of telomere length.

Pt-ttpy is a metallo-organic compound and an effective G-quadruplex ligand that efficiently induces significant telomere-associated DNA damage in cancer cells by inhibiting telomerase and/or telomere function. It also causes various chromatin abnormalities during mitosis, such as chromatin bridges, ultrafine bridges (UFB), and double-stranded breaks (DSB).