foxo1

Oxypaeoniflorin a monoterpene glycoside compound isolated from Paeoniae, is an antioxidant, is neuroprotective and anti-inflammatory.

Marein shows neuroprotective effect on PC12 cell damage induced by methylglyoxal, which is due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway, it may be a potent compound for preventing/counteracting diabetic e

Kihadanin B can repress the adipogenesis by decreasing lipid accumulation through the suppression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes.

FOXO1-IN-3 is a highly-selective, orally active inhibitor of FOXO1 that reduces hepatic glucose production and improves insulin sensitivity and glucose regulation in db/db mice, without causing weight gain [1].

AS1842856 is a Foxo1 inhibitor (IC50=30 nM) that specifically blocks the transcriptional activity of Foxo1 and reduces its activity by directly binding to activated FoxO1. AS1842856 has autophagy inhibitory activity.

JY-2 is an orally active and selective forkhead transcription factor O1 (FoxO1) inhibitor with antidiabetic activity and inhibits FoxO1 transcription.JY-2 can be used to study psoriasis and diabetes.

PFI-90, a selective histone demethylase (KDM3B) inhibitor, targets PAX3-FOXO1 action and demonstrates potential antitumor activity. It induces apoptosis and myogenic differentiation, leading to increased cell death.

LOM612 is a potent and specific FOXO relocator that induces nuclear translocation of the FOXO3a reporter protein as well as endogenous FOXO3a and FOXO1 in a dose-dependent manner in U2OS cells, down-regulates the expression of c-Myc and cyclin D1, and has anti-proliferative effects in human cancer cell lines.

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

Lipase, triacylglycerol (Alkaline lipase) is a specific enzyme that plays an important role in the catabolism of triacylglycerol to glycerol and fatty acids and is required for the transfer of fatty acids to various tissues of the body, and whose transcriptional receipt of transcripts is subjected to nutrient/hormonal regulation and is capable of being upregulated by PPARγ,TNFα downregulation, and insulin-mediated downregulation of FOXO1 nuclear localization.

MIR96-IN-1 selectively inhibits biogenesis of microRNA-96, upregulating a protein target (FOXO1) and inducing apoptosis in cancer cells.

Euphjatrophane M (Compound 6) is a FOXO1 inhibitor that reduces NF-κBp65 phosphorylation and exhibits anti-inflammatory properties. It can inhibit the production of nitric oxide and also suppress the mRNA expression of IL-6, IL-1β, and TNFα in LPS-induced RAW 264.7 macrophages.

ROCK2-IN-13 is a selective inhibitor of ROCK2. It functions by hindering ROCK2 kinase activity and reducing its nuclear expression, consequently disrupting the interaction between ROCK2 and transcription co-activators p300 and PGC 1α, thereby suppressing oncogene transcription. ROCK2-IN-13 activates FOXO1-driven PTEN expression, which in turn inhibits the PI3K/Akt pathway, induces G2/M cell cycle arrest, and promotes apoptosis (apoptosis). This compound effectively eliminates the nuclear transcription function of ROCK2 that maintains oncogenic signaling and restores the tumor-suppressive PTEN/FOXO1 axis. ROCK2-IN-13 is utilized in prostate cancer research.

SB 699551 is a selective 5-HT5A antagonist (Ki=6.31 nM) that enhances 5-HT neuronal function. It inhibits SERT (Ki=25.12 nM), reduces phosphorylation levels of AKT and FOXO1, and exhibits inhibitory effects against breast cancer.

AS1708727 is an orally bioavailable FOXO1 inhibitor that reduces plasma glucose and triglyceride levels in diabetic mice.

α-Lipoic Acid sodium (Thioctic acid sodium) is an antioxidant and essential cofactor for mitochondrial enzyme complexes. It inhibits NF-κB-dependent HIV-1 replication, induces endoplasmic reticulum stress-mediated apoptosis in hepatocellular carcinoma cells, and modulates SREBP-1, FOXO1, and Nrf2 to improve high-fat diet-induced hepatic steatosis.

Acetyl-Exenatide, an acetylated derivative of Exenatide, mirrors insulin's functionality and is utilized in type 2 diabetes research. It promotes Th17 differentiation, inhibits Tregs differentiation, and downregulates PI3K/Akt/FoxO1 phosphorylation [1].

Kushenol I is a bioactive compound exhibiting anti-inflammatory, antioxidant, and ulcerative colitis–ameliorating effects, demonstrated in a DSS-induced UC mouse model where oral administration improved colon length, body weight, and disease scores while reducing pro-inflammatory cytokines including IL-1β, IL-6, IL-17, and TNF-α. Kushenol I increase IL-10 expression, inhibited key inflammatory signaling proteins such as AKT, p38 MAPK, PI3K, NLRP3, FOXO1, and TLR4, enhancing intestinal barrier integrity. Kushenol I positively modulate gut microbiota, and elevated splenic T-cell proportions, supporting therapeutic potential in inflammatory bowel disease.