drosophila

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

AGK7 is an inactive control of AGK2, a selective SIRT2 inhibitor that selectively inhibits SIRT3 over SIRT1 and SIRT2 (IC50 = >5 μM, >50 μM and >50 μM for SIRT3, SIRT1, and SIRT2, respectively).

Thiacloprid is a neonicotinoid insecticide that acts as a selective agonist at insect nicotinic acetylcholine receptors (nAChRs) with IC50values of 2.7 and 860 nM forDrosophilanAChRs and M10 mouse fibroblast cells expressing α4β2 subunit-containing nAChRs, respectively.1It is active against aphids, whiteflies, various species of beetle, andLepidopteraspecies when used at concentrations ranging from 48 to 180 g AI/hectare.2It has anti-estrogenic activity in a yeast estrogen screen and is toxic to adult female houseflies and mice (LD50s = 0.03 and 28 mg/kg, respectively).1,3Formulations containing thiacloprid have been used in the control of insects in agriculture. 1.Tomizawa, M., and Casida, J.E.Selective toxicity of neonicotinoids attributable to specificity of insect and mammalian nicotinic receptorsAnnu. Rev. Entomol.48339-364(2003) 2.Elbert, A., Erdelen, C., Kuhnhold, J., et al.Thiacloprid, a novel neonicotinoid insecticide for foliar applicationProc. Brighton Crop. Prot. Conf. - Pests and Diseases121-26(2000) 3.Westlund, P., and Yargeau, V.Investigation of the presence and endocrine activities of pesticides found in wastewater effluent using yeast-based bioassaysSci. Total Environ.607-608744-751(2017)

SecinH3 is selective cytohesin inhibitor.

Moxnidazole, a 5-nitroimidazole, is mutagenic in microbial assays and in Drosophila, inducing genetic alterations in mouse somatic cells.

Chlorantraniliprole (Rynaxypyr) is an insecticide. Chlorantraniliprole potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC50, 14 μM).

Lotilaner is an anthelmintic agent and a non-competitive GABA_A receptor antagonist with an IC₅₀ value of 23.84 nM for Drosophila GABA receptors. Lotilaner selectively acts on the nervous system of invertebrates to exert its anthelmintic effect and exhibits no significant affinity for mammalian GABA_A receptors.

AChE/BChE-IN-25 (Compound 6e) is an orally active inhibitor of hAChE and eqBChE, with IC50 values of 7.9 nM and 0.79 nM, respectively. This compound exhibits antioxidant activity, effective in scavenging free radicals with an IC50 of 22.91 μM. AChE/BChE-IN-25 demonstrates neuroprotective effects by reducing mitochondrial and cellular oxidative stress in a Drosophila Alzheimer's model and improves spatial and cognitive memory impairments induced by Scopolamine in mouse models.

GABA receptor antagonist 2 (Compound IId) is a GABA receptor blocker with an LC50 of 0.0735 μg/mL against Plutella xylostella (P. xylostella). This compound exhibits significant insecticidal activity against P. xylostella and its resistant strains, as well as against Spodoptera frugiperda and Chilo suppressalis. GABA receptor antagonist 2 can bind to the GABA receptor at the Drosophila RdlG335 site and is useful for managing resistant pest populations.

AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numero

Xanthumin is a naturally occurring insect development inhibitor against Drosophila melanogaster. Xanthumin is also an antibacterial compound.

Neomyosuppressin is a myoinhibiting neuropeptide isolated from the grey fleshfly, Neobellieria bullata and Drosophila.

Auten-99 HBr (Auten-99) is a myotubularin phosphatase Jumpy inhibitor exerting potent neuroprotective effects. AUTEN-99 activates autophagy in cell cultures and animal models. AUTEN-99 appears to effectively penetrate through the blood-brain barrier, and impedes the progression of neurodegenerative symptoms in Drosophila models of Parkinson's and Huntington's diseases. Furthermore, the molecule increases the survival of isolated neurons under normal and oxidative stress-induced conditions. Thus, AUTEN-99 serves as a potent neuroprotective drug candidate for preventing and treating diverse neurodegenerative pathologies, and may promote healthy aging.

ML207 inhibits lipid storage in Drosophila melanogaster.

OptoDArG is an optogenetic tool compound used to reversibly regulate DAG (diacylglycerol)-related signaling pathways under specific light conditions. It acts as a potent agonist of lipid-gated ion channels (TRPC3/6/7), mimicking the activating function of endogenous DAG, and can also be used to study DAG-dependent activation of TRPL channels in Drosophila as well as the photocapacitive effect resulting from membrane-bound photoisomerization.

Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001). Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4 References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001).

Ceramide phosphoethanolamine (CPE) is an analog of sphingomyelin that contains ethanolamine rather than choline as the head group. It is the principal membrane phospholipid in invertebrates such as Drosophila, which lacks sphingomyelin. It is only produced in small amounts in mammalian cells, accounting for approximately 0.02 mol% of total phospholipids in mouse testis and brain. In Drosophila, CPE is biosynthesized by CPE synthase from ceramide and cytidine diphosphate-ethanolamine in the Golgi lumen. In mammals, it is biosynthesized by sphingomyelin synthase 2 (SMS2) in the plasma membrane and by sphingomyelin synthase-related protein (SMSr) in the endoplasmic reticulum (ER). In Drosophila, CPE has a role in glial ensheathment of axons. Disrupting CPE synthesis by depleting SMSr in vitro in mammalian cells leads to an accumulation of ER ceramides, which are then mislocalized to the mitochondria, inducing apoptosis. However, ceramide levels are not altered in transgenic mice lacking SMSr catalytic activity. CPEs (bovine) is a mixture of CPEs with variable N-acyl chain lengths.

C2 Ceramide (d14:1/2:0) is a bioactive sphingolipid that, when administered dietarily at 100 μM, induces lipotoxic cardiomyopathy by increasing diastolic and systolic diameter, reducing fractional shortening, and decreasing the number of normal cardiac contractile events in Drosophila.

Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), specifically inhibiting it in a dose-dependent manner while exhibiting minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. At 40 μM, Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells and prevents the assembly of a contractile ring during cell division in Drosophila S2 cells, but it does not affect ring ingression, indicating that Aurora B kinase activity is not required for that process.

9(Z)-Tricosene is a long-chain monounsaturated alkene (C23:1) containing a cis double bond. 9(Z)-Tricosene is commonly used as a component of insect pheromones and plays a particularly important role in sexual communication among insects such as fruit flies. 9(Z)-Tricosene is widely used in chemical ecology research and in experimental analyses of insect behavioral regulation mechanisms.

Potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells. Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID:24900436 |Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID:27461445 |Giordani et al (2016) The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 7 55313 PMID:27486815

Unsaturated, long-chain hydrocarbons are found on the cuticles of insects and can act as pheromones. In mature Drosophila melanogaster, certain cuticular hydrocarbons are sexually dimorphic: males synthesize 23- and 25-C monoenes and females produce 27- and 29-C dienes. Each of these lipids plays specific roles in regulating male sexual behavior, with dienes stimulating courtship. 7(Z),11(Z)-Pentacosadiene is a 25-C hydrocarbon that is found in low abundance on cuticles of mature Drosophila females. Depletion of a female-specific elongase (eloF), which leads to an increase in 7(Z),11(Z)-pentacosadiene along with a parallel decrease in 7,11-nonacosadiene, significantly reduces copulation in Drosophila. This raises the possibility that 7(Z),11(Z)-pentacosadiene may act as an anti-aphrodisiac.

7(Z)-Pentacosene is an unsaturated cuticular hydrocarbon that acts as a contact sex pheromone in fruit flies. In different species and genotypes of Drosophila, it can be found on both males and females. Pentacosene may stimulate copulation either by itself at high concentrations or when combined with other alkenes. Interestingly, the absolute level of pentacosene increases in Drosophila females immediately after copulation.

7(Z)-Tricosene is an insect pheromone and endogenous metabolite for mating and interspecific recognition.