c. elegans

2-Bromohexadecanoic acid (2-BP) is a non-metabolizable palmitate analog, an agonist of PPARδ, which acts as a palmitoylation inhibitor and inhibits DHHC-mediated palmitoylation.

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.

Dafadine-A is an analog of dafadine and a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans. Mammalian orthologs that also inhibit DAF-9 (CYP27A1).

HDAC6-IN-49 (Compound 3) is an inhibitor of HDAC, with IC50 values of 0.012 and 0.735 µM against HDAC6 and HDAC1, respectively. Additionally, it inhibits MAO-B, cholinesterase (ChE), histamine receptor (H3R), and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective effects in SH-SY5Y cells and enhances cognitive functions and motor abilities in fruit fly models of Parkinson's disease and C. elegans models of Alzheimer's disease.

Antibiofilm agent-12 (Compound C13), an antifungal belonging to the carbamate derivatives, exhibits significant antifungal activity against Candida auris, with an MIC90 of 237.9 μM. It inhibits the drug efflux pump activity of Candida auris and promotes ergosterol depletion, thereby hindering the formation of Candida auris biofilms and reducing its metabolic flexibility. Additionally, Antibiofilm agent-12 demonstrates antifungal efficacy in a C. elegans model following Candida auris infection.

Antibiofilm agent prodrug 1 (Compound 5c) demonstrates antibacterial properties by inhibiting biofilm formation and iron uptake. It effectively suppresses Pseudomonas aeruginosa PAO1 with a minimum inhibitory concentration (MIC) of 1.07 μM. In addition, Antibiofilm agent prodrug 1 exhibits anti-infective activity in Caenorhabditis elegans, enhancing the survival rate of the nematodes.

JX10 is an anti-aging agent. It suppresses the expression of p38 MAPK and NF-κB. JX10 demonstrates significant anti-aging effects in C. elegans, senescent cells, and aged mice.

Nemadipine A is an L-type calcium channel blocker that induces morphological and growth defects in wild-type C. elegans and those with hypoexpression of egl-19, which encodes the only L-type calcium channel α1-subunit in the C. elegans genome. It also inhibits L-type calcium channels in chick ciliary neurons. Nemadipine A increases TRAIL-induced cytotoxicity and synergistically enhances caspase-8 and caspase-3 activation in a concentration-dependent manner in H1299 lung adenocarcinoma cells. It also decreases Survivin expression when used alone or in combination with TRAIL in A549 cells.

Milbemycin A3 is a member of a complex family of macrocyclic lactones that contain a characteristic spiroketal group produced from the fermentation of soil bacterium S. hygroscopicus subsp. aureolacrimosus. As a compound that potentiates glutamate and GABA-gated chloride-channel opening, milbemycin A3 is used as a nematocide and insecticide. The acaricidal and nematocidal activity of a mixture of milbemycin A3 and milbemycin A4 against adult spider mites, spider mite eggs, and C. elegans are reported at IC50 values of 5.3, 41.1, and 9.5 μg/ml.

Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a . It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.

Avermectin B1a monosaccharide is a macrolide anthelmintic and monosaccharide form of avermectin B1a . It is lethal to C. elegans with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a monosaccharide also stimulates conductance in isolated shore crab muscle.

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay. [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample - Signallow)/(Signalhigh - Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.

Paraherquamide A is a mycotoxin anthelmintic originally isolated from P. paraherquei. It binds to acetylcholine receptors (IC50 = 0.5 nM for head homogenates of M. domestica) and acts as an antagonist. Paraherquamide A is toxic to C. elegans (LD50 = 2.5 μg/ml) and effective against T. colubriformis infection in gerbils when used at doses ranging from 0.39 to 200 mg/kg. It is toxic to mice (LD50 = 14.9 mg/kg).

Paraherquamide E is a fungal metabolite originally isolated from P. charlesii with anthelmintic and insecticidal activities. It is lethal to C. elegans [LD50 = 6 μg/ml] and O. fasciatus [LD50 = 0.089 μg/nymph]. Oral administration of paraherquamide E [0.5-4 mg/kg] reduces T. colubriformis fecal egg count in gerbils.

CAY10711 is a substituted diamine that produces rapid bactericidal activity against both Gram-positive and Gram-negative bacteria, including methicillin-resistant S. aureus (MRSA) and stationary-phase bacteria. It displays MIC99 values of 2.9, 11.5, 2.9, and 2.9 μM against S. aureus RN4220, P. aeruginosa PAO1, E. coli ANS1, and MRSA 10082B, respectively. CAY10711 reduces biofilm formation and promotes biofilm dispersal in P. aeruginosa. It is synergistic with kanamycin and has limited adverse effects against mammalian cells or C. elegans development, survival, or reproduction.

Cholera autoinducer 1 is an autoinducer of Vibrio cholerae. Cholera autoinducer 1 influences chemotaxis in C. elegans [1].

5-Ph-IAA-AM, an eggshell-permeable analog of 5-Ph-IAA, enhances protein degradation in laid embryos and can be used to reveal the roles of temporally controlled protein degradation in C. elegans embryogenesis and development [1].

Magnesium Oxaloacetate is an inhibitor of the amebicidal activity of activated murine macrophages, helping the parasite to survive within the mouse large intestine and increasing the survival of C. elegans exposed to H2O2.

Vinclozolin M2, an active metabolite of vinclozolin, is generated through successive esterase activity and decarboxylation in C. elegans, as well as decarboxylation in human liver microsomes. It functions as an antagonist to the mineralocorticoid (IC50= 1,400 nM) and androgen receptors (IC50= 0.17 nM), demonstrated in reporter assays with MCF-7 cells. This compound is exclusively sold for research and analytical purposes, tailored for controlled laboratory use, and is not available in bulk sizes.

1,2,3-Tritridecanoyl glycerol, a synthetic triacylglycerol featuring tridecanoic acid at the sn-1, sn-2, and sn-3 positions, serves as a standard for relative triacylglycerols quantification in C. elegans fat stores and as an internal standard in quantifying triacylglycerols in serum and liver of adult rat offspring exposed to dietary conjugated linoleic acids during and post-gestation.

Alloaromadendrene, an antioxidant isolated from the leaves of mixed-type C. osmophloeum, protects C. elegans against oxidative stress induced by walnut quinone and prolongs the life of C. elegans [1].

Cyprocide-B is activated by Cytochrome P450, which converts it into an electrophilic metabolite that selectively kills the nematode C. elegans. This compound holds promise for research into selective nematicidal agents.

Tomatidine serves as an anti-inflammatory agent by inhibiting NF-κB and JNK signaling pathways. Additionally, it induces autophagy in both mammalian cells and C. elegans.

Lappaol A has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol A also has potential chemosensitizing activity, it may be candidates for developing novel adjuvant an