foxo

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.

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].

FOXO4-DRI acetate is a bioactive chemical.

Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

Sulfoxone sodium ( Adesulfone Sodium) is an anti-leprosy drug.

Umifoxolaner is an anti-parasitic agent (veterinary).

FOXO4-DRI, a cell-permeable peptide antagonist, inhibits the interaction between FOXO4 and p53. It functions as a senolytic peptide, promoting apoptosis in senescent cells [1].

Afoxolaner (Standard) is the standard substance of Afoxolaner, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

Broussochalcone A is a natural antioxidant and xanthine oxidase inhibitor (IC50 = 2.21 μM) that scavenges free radicals, inhibits iron-induced lipid peroxidation, and reduces nitric oxide synthesis in LPS-activated macrophages. Broussochalcone A induces apoptosis in human renal carcinoma cells by increasing ROS levels and activating the FOXO3 signaling pathway. Broussochalcone A is also a novel NR4A1 inhibitor that induces apoptosis in pancreatic cancer cells through NR4A1-dependent pathways.

BN201 (OCS-05) is a drug with neuroprotective and myelin repair effects, which acts mainly by activating serum glucocorticoid kinase-2 (SGK2), which in turn activates the FOXO3 pathway to promote neuronal survival and myelin repair. It is mainly used for the treatment of inflammatory neurological diseases such as multiple sclerosis (MS) and experimental autoimmune encephalomyelitis (EAE).BN201 is able to regulate multiple kinases in the insulin growth factor 1 (IGF1) pathway and cross the blood-brain barrier.

SB 699551 dihydrochloride is a 5-ht5a receptor antagonist.

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.

kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activation.

D-chiro-Inositol (D-(+)-CHIRO-INOSITOL) is an epimer of myo-inositol that is found in certain mammalian glycosylphosphatidylinositol protein anchors and inositol phosphoglycans possessing insulin-like bioactivity.

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.

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.

anticancer

Chlorzoxazone (Chlorzoxazon) is a Muscle Relaxant. The physiologic effect of chlorzoxazone is by means of Centrally-mediated Muscle Relaxation.

RLX (PD 139530) is a PI3K/Akt/FoxO3a signal inhibitor with anticancer activity against tumour cell lines such as colon cancer, inducing sub-G1 arrest and mitochondrial potential loss, thereby inhibiting tumour growth. RLX also exhibits antitussive and anti-asthmatic activity, reducing eosinophils and total lymphocytes in bronchoalveolar lavage (BAL) fluid, and exhibits toxicity toward A549 cells.

RLX HCl is a narcissus ketone analogue with anticancer activity that inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a signalling pathway in experimental colon cancer, downregulating the p110α and p85 subunits of PI3K in HCT-116 cells, and exhibiting antiproliferative effects.

FOXJ1 agonist 1 (compound 16c), an orally effective small molecule, effectively enhances FOXJ1 expression and acts on multiciliated cells (MCC) in the mammalian airway system to prevent chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 induces motile cilia production in the respiratory system of both zebrafish and mammals and inhibits elastase-induced COPD in mouse models. Additionally, Foxj1-IN-1 demonstrates good liver microsomal stability and favorable in vivo pharmacokinetic (PK) curves and area under the curve (AUC). It exhibits negligible inhibition of CYP and hERG and lacks significant cytotoxicity.

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.

Conessine (Conessinum), a steroidal alkaloid isolated from Holarrhena floribunda, interacts with the histamine H3 receptor and has anti-malarial activity.

Piperacetazine (Piperacetazinum), an antipsychotic prodrug, is used forschizophrenia.