zebrafish

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

Zebrafish Kisspeptin-1 is the core sequence of the neuropeptide kisspeptin-1, which plays a crucial role in regulating the release of gonadotropin-releasing hormone (GnRH) and modulating the reproductive system.

Kisspeptin-10, a neuropeptide present in the brains, ovaries, and testes of zebrafish, plays a critical role in gonadal development and steroid expression. At a concentration of 10 ng/ml, it enhances the mRNA levels for the luteinizing hormone (Lh) receptor and both progestin receptor a (Pra) and Prb in zebrafish ovarian follicles. In female goldfish, doses of 0.1 and 1 µg/g of Kisspeptin-10 elevate serum levels of luteinizing hormone, with no similar effect observed in male goldfish.

Oxazolone has been used as a haptenizing agent to induce inflammatory responses in intestinal tissue of adult zebrafish and as a model for gene expression studies in two forms of inflammatory bowel disease, such as Crohn's disease and ulcerative colitis.

G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) agonist that promotes glucose-6-phosphate dehydrogenase (G6PD) oligomerization to a catalytically competent form. G6PD activator AG1 reduces oxidative stress in cells and zebrafish, reduces chloroquine or diamide-induced oxidative stress in human erythrocytes, and can be used to study glucose-6-phosphate dehydrogenase deficiency.

Diphenyl Phosphate is capable of gender-specific inhibition of growth and energy metabolism in zebrafish.

Metalaxyl (CGA 48988) is a widely used fungicide that inhibits protein synthesis in fungi, interferes with skeletal development in zebrafish embryos, and can be used to control plant diseases caused by oomycetous fungi.

Dibutyl phthalate (1,2-Benzenedicarboxylic acid) is a plasticizer, commonly used in industrial manufacturing, that causes cardiac damage by disrupting Ca(2+) transfer from the endoplasmic reticulum to the mitochondria and triggering subsequent cellular death.Dibutyl phthalate induces oxidative damage in the brain of zebrafish.

Pyriproxyfen (S-31183) is an insecticide that acts as a biomimetic of juvenile hormone.

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1 2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

Qingyangshengenin B (Otophylloside B) is a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic and anti-aging effects, it can extend lifespan, increase heat stress-resistance, delay body paralysis, and increase the chemotaxis response in C. elegans models of Alzheimer's disease. Otophylloside B can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1 CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro5-3335 also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.

MitoBloCK-11 (MB-11) is a s mall molecule inhibitor of mitochondrial protein import possibly acts through transport protein Seo1, but not Tom70 or Tom20; inhibits precursor proteins that contain hydrophobic segments, confers growth in media lacking uracil in a specific manner and affects zebrafish development.

Otophylloside F can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.

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.

MHLWAAK, an antioxidant peptide derived from pancreatin hydrolysate of C-phycocyanin, exhibits potent DPPH and ABTS radical scavenging capabilities. It effectively shields zebrafish larvae against H2O2-induced oxidative damage [1].

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg L. This compound also exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg adult) and low toxicity to zebrafish (LC50: 42.4 mg L) [1].

Fedovapagon (VA106483) is a selective and potent agonist of the vasopressin V2 receptor (V2R) that inhibits the growth of intersegmental vessels in zebrafish. It can be used to study overactive bladder, nocturia, and painful bladder syndromes.

Pentacosafluorotridecanoic Acid (PFTrDA) is a perfluoroalkyl substance (PFAS) that exhibits various biological impacts across different species. In zebrafish embryos, exposure to PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, at concentrations of 0.1 and 0.3 mg L. At a dosage of 10 mg kg, PFTrDA reduces serum testosterone and luteinizing hormone levels, as well as palmitic acid, linoleic acid, and oleic acid levels in the testicular interstitial cells of late adolescent rats. In humans, maternal plasma levels of PFTrDA during pregnancy are positively correlated with the development of eczema in female infants (but not male infants), and PFTrDA levels are higher in the livers of cancerous humans compared to non-cancerous ones. Additionally, PFTrDA is found in marine mammals.

Vinaginsenoside R4 was isolated from the leaves of hydroponically grown ginseng. It inhibits melanin biosynthesis and enhances pigmentation in zebrafish without any cytotoxic effects on melan-a cells. It may have potential as a new skin whitening compound.

Fenobucarb, a widely employed carbamate insecticide, poses potential risks to the cardiovascular and cerebrovascular systems in animals[1][2]. It triggers developmental neurotoxicity in zebrafish by engaging pathways related to inflammation, oxidative stress, degeneration, and apoptosis.

Nifurpirinol (P-7138) is an antimicrobial compound that is acutely toxic to milkfish (Chanos chanos) species. Nifurpirinol selectively disrupts the activity of collagen-producing 1alpha2 cells in the Fli colRN zebrafish line.

AP-III-a4 (ENOblock) (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.

MDYYFEER TFA, an antioxidant peptide derived from pancreatin hydrolysate of C-phycocyanin, exhibits potent DPPH and ABTS radical scavenging capability. This compound effectively shields zebrafish larvae against oxidative damage induced by H2O2 [1].