drosophila

Selisistat (EX-527) 是一种去乙酰化酶 SIRT1 的抑制剂 (IC50=38 nM)，具有有效性和特异性。Selisistat 可以用于神经系统疾病如亨廷顿舞蹈病的研究。

AGK7 是 sirtuin 2 (SIRT2) 抑制剂。它在体外和帕金森病果蝇模型中均能抑制多巴胺能细胞的凋亡。在帕金森病细胞模型中，它改善了 α-突触核蛋白毒性和修饰的包涵体形态

Thiacloprid 属于氯烟碱类杀虫剂，主要用于防治蔬菜和果园中的蚜虫。它会破坏 DNA 的稳定性，通过疏水或氢相互作用，结合到小沟槽中，改变 DNA 的结构和稳定性。

Moxnidazole 是一种5-硝基咪唑，在微生物试验和果蝇中具有诱变性，诱导小鼠体细胞的遗传改变。

Chlorantraniliprole (Rynaxypyr) 是一种杀虫剂，能够有效地、选择性地激活鱼尼丁受体 (ryanodine receptor)，对黑腹果蝇和烟芽夜蛾的 ryanodine 受体 EC50 值分别为 40 nM 和 50 nM，对其选择性是对小鼠骨骼肌 2C12 细胞 ryanodine 受体 (EC50，14 μM) 的 300 多倍。

Auten-99 HBr (Auten-99) 是新型肌管蛋白磷酸酶 Jumpy( MTMR14) 的抑制剂，可通过血脑屏障，具有强大的神经保护作用。

Antennapedia Peptide TFA (188842-14-0 free base) 是一种 16 个氨基酸的肽，是细胞穿透肽家族的成员，最初来源于果蝇转录因子 Antennapedia 的 60 个氨基酸长的同源域。

Penetratin is a peptide derived from the amphiphilic Drosophila Antennapedia homeodomain.

Lapachol (CI75490) 是从Tabebuia avellanedae 中分离得到的一种萘醌。它具有具有抗菌、抗炎、镇痛、抗肿瘤和抗生素特性。

Milbemectin is composed of 30% milbemycin A3 and 70% milbemycin A4, exhibiting acaricidal and nematocidal properties effective against adult spider mites, their eggs, and C. elegans, with IC50 values of 5.3, 41.1, and 9.5 µg ml, respectively. It functions as an allosteric agonist of the Drosophila RDL GABA receptor, and demonstrates efficacy against the pinewood nematode, B. xylophilus, with an LC20 of 0.0781 mg liter.

ML207 inhibits lipid storage in Drosophila melanogaster.

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. Dietary administration of C2 ceramide (d14:1 2:0) (100 μM) induces lipotoxic cardiomyopathy via increasing diastolic and systolic diameter as well as reducing fractional shortening and the number of normal cardiac contractile events in Drosophila.

6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive wing position defects in a Drosophila model of oculopharyngeal muscular dystrophy (OPMD) when larvae are raised on medium containing doses ranging from 300 to 400 μM and in adults following dietary administration of 1-3 mM doses. 6-Aminophenanthridine also reduces muscle degeneration and decreases the number of nuclear inclusions in thoracic muscle in a Drosophila model of OPMD.

Antennapedia Peptide is a 16 amino acid peptide corresponding to the region within the Drosophila Antennapedia DNA binding domain that is mapped to be responsible for cellular internalization.

CP681301 是CDK5的有效抑制剂，具有抗增殖活性。CP681301 在果蝇中表现出抗肿瘤活性。CP681301 降低神经胶质瘤干细胞中 CD133、OLIG2、SOX2、KI67、pCDK5 蛋白水平的表达。CP681301 减少小鼠胶质瘤异种移植物的自我更新。

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.

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

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

Rediocide A, an insecticide, can inhibit calcium mobilization in Drosophila G-protein- coupled receptors (GPCR)s other than methuselah, it can induce GPCR desensitization and internalization, and such effects are mediated by the activation of conventional

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

Andropin为特异于雄性的抗菌肽，源自黑腹果蝇。

C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s = 25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6 2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6 2 transgenic mouse model of Huntington's disease.

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