senescence

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

Milademetan (DS-3032) is an orally active and potent MDM2 inhibitor with antitumor activity that induces G1 cell cycle arrest, senescence, and apoptosis.Milademetan is used in the study of acute myeloid leukemia and solid tumors.

RH1 (NSC 697726) is a bioreductive anticancer compound that exhibits dose-dependent biphasic effects in vitro, inducing apoptosis at higher doses and senescence at lower doses.

p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase (IC50 = 35 nM). It inhibits senescence induced by the oncogene RAS.

Royal Jelly Acid (Queen Bee Acid) is a major fatty acid found in royal jelly that promotes neuronal growth and protection and reduces anxiety. Royal Jelly Acid induces reactive oxygen species (ROS)-mediated apoptosis in A549 cells, improves non-alcoholic fatty liver disease by activating the AMPK-α signaling pathway, and reduces bone loss by inhibiting the NF-κB signaling pathway downstream of FFAR4. Royal Jelly Acid also exhibits inhibitory effects against various bacteria and fungi, including Aspergillus niger, mold, and Staphylococcus aureus. By targeting aspartyl β-hydroxylase and inhibiting chondrocyte senescence, Royal Jelly Acid exerts a preventive and therapeutic effect against osteoarthritis.

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence, and mitotic catastrophe in human cancer cells.

BRD4770, a histone methyltransferase G9a inhibitor, induces cell senescence.

FAPy-adenine (4,6-diamino-5-N-formamidopyrimidine) is an oxidised DNA base, and its levels in the brains of Alzheimer's disease patients show an upward trend.

SLCB050 is a compound with anticancer activity that inhibits the interaction between DX2 and p14/ARF. It decreases the viability of human lung cancer cells, particularly small cell lung cancer cells, in a p14/ARF-dependent manner, and induces cell apoptosis (apoptosis) and senescence.

STAT3-IN-31 (compound K2071), derived from STATtic, acts as an inhibitor of both STAT3 and mitotic processes. This compound interrupts mitotic progression and impacts the formation of the mitotic spindle. Additionally, STAT3-IN-31 hampers migration in glioblastoma cells, suppresses cellular proliferation within tumor spheroids, induces senescence in glioblastoma, and inhibits the growth of Temozolomide-resistant cells while reducing the secretion of the pro-inflammatory cytokine monocyte chemoattractant protein (MCP-1).

GTSE1-IN-1 (compound Y18), an orally active GTSE1 inhibitor, exhibits notable anticancer properties. It effectively represses the proliferation of cancer cells by downregulating GTSE1 transcription and expression, which leads to DNA damage and promotes persistent cell cycle arrest and cellular senescence. Moreover, GTSE1-IN-1 substantially reduces the adhesion, migration, and invasion of colorectal cancer HCT116 cells and non-small cell lung cancer A549 cells in vitro.

MRTF-A-IN-2 (compound 16) is an inhibitor of MRTF-A. It effectively suppresses cell proliferation and induces senescence in HCC cells.

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.

MRTF-A-IN-1 (compound 14) is an inhibitor of MRTF-A. It effectively suppresses cell proliferation and induces senescence in HCC cells.

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.

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.

GL392 is a senolytic agent that delivers the potent senescence-clearing compound Dasatinib specifically to senescent cells. By targeting the LBD domain, it binds lipofuscin in these cells and releases Dasatinib via an ester linkage, inducing apoptosis (Apoptosis) in senescent cells. Additionally, GL392 is encapsulated in PEO-b-PCL microcapsules to ensure efficient intracellular delivery while minimizing systemic toxicity. GL392 is applicable in cancer research.

CDK2-IN-44 (Compound 46) is an inhibitor of cyclin-dependent kinase 2 (CDK2). It effectively suppresses the proliferation of cancer cells by arresting the cell cycle, promoting apoptosis (Apoptosis), and inducing cellular senescence. This compound shows potential in research related to ovarian and breast cancers.

HSP90α-IN-1 is an HSP90α inhibitor (IC50= 111 nM) that demonstrates anti-aging activity across various cellular senescence models. Belonging to the xanthine family, HSP90α-IN-1 is involved in research focused on combating age-related inflammation, senescence, and diseases (including cancer), and it may contribute to extending healthy lifespan.

Anticanceragent 205 (compound 9) is an effective anticancer agent that binds to the G4-mtDNA target, inhibiting the replication, transcription, and translation of mtDNA (mitochondrial genome). It induces mitochondrial dysfunction, increases ROS production, and triggers DNA damage and cellular senescence. Anticanceragent 205 also promotes apoptosis and causes cell cycle arrest at the G0/G1 phase, showing potential for research in colorectal cancer.

SL-IN-1 (Compound C6) is an inhibitor of plant hormone steroidal lactone (SL) receptors. It enhances rice tillering, inhibits the germination of root parasitic plant P. aegyptiaca seeds (IC50 is 82.8 µM), delays darkness-induced senescence in rice leaves, and protects leaf membranes from lipid peroxidation.