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29

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22026	AGK7	Others; Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair; Others
	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
T6111	Selisistat EX-527,司来司他,SEN0014196	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	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。
T68110	Moxnidazole
	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。
TP1318	Antennapedia Peptide TFA(188842-14-0 free base) Antennapedia Peptide(TFA)	Others	Others
	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。
T15775	Lotilaner	GABA Receptor; Parasite	Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	Lotilaner 是杀寄生虫剂，是非竞争性的昆虫GABACl 受体拮抗剂，对果蝇 GABA 受体的IC50值为 23.84 nM。对家犬的 GABAA 无明显作用。
T26684	Auten-99 HBr Auten-99,Auten-99 hydrochloride. Auten-99 HBr,Auten99,Auten 99	Phosphatase	Metabolism
	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。
T60127	Chlorantraniliprole Rynaxypyr,Chlorantranilipole,Rynaxpyr	Others	Others
	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。
T41087	Penetratin
	Penetratin is a peptide derived from the amphiphilic Drosophila Antennapedia homeodomain.
T25862	Neomyosuppressin Thr-asp-val-asp-his-val-phe-leu-arg-phenh2,Dromyosuppressin,Neb-MS
	Neomyosuppressin is a myoinhibiting neuropeptide isolated from the grey fleshfly, Neobellieria bullata and Drosophila.
T28064	ML207 ML 207,LLI01-022,ML-207
	ML207 inhibits lipid storage in Drosophila melanogaster.
T80399	Andropin
	Andropin为特异于雄性的抗菌肽，源自黑腹果蝇。
T40644	DL-Leucyl-DL-phenylalanine
	DL-Leucyl-DL-phenylalanine, a dipeptide, serves as a substrate for detecting two distinct regions of dipeptidase staining on gels in both Drosophila simulans and Drosophila melanogaster.
T36801	Binucleine 2
	Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division ...
T37922	7(Z),11(Z)-Pentacosadiene
	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 fema...
TP1840	Antennapedia Peptide
	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.
T37923	7(Z)-Pentacosene
	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.
T36188	Ceramide Phosphoethanolamines (bovine)
	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...
T36230	C2 Ceramide (d14:1/2:0) C2 Ceramide (d14:1/2:0)
	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.
T22552	AD57 (hydrochloride)	Others	Others
	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
T71552	ASC-JM-17
	ASC-JM-17 is an activator of both Nrf1 and Nrf2 proteins. ASC-JM17 acts on Nrf1, Nrf2 and Hsf1 to increase the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. ASC-JM17 ameliorates toxicity of the mutant androgen receptor (AR) responsible for SBMA in cell, fly and mouse models. Knockdown of the Drosophila Nrf1 and Nrf2 ortholog cap ‘n’ collar isoform-C, but not Hsf1, blocks the protective effect of ASC-JM17 on mutant AR-induced eye degeneration in flies.
T38187	6-Aminophenanthridine
	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 w...
T6664	SecinH3	Apoptosis	Apoptosis
	SecinH3 是cytohesins 的拮抗剂，是选择性细胞粘附素抑制剂。对于hCyh1、hCyh2、mCyh3、hCyh3、果蝇和yGea2-S7的IC50值分别为 5.4 μM、2.4 μM、5.4 μM、5.6 μM、5.6 μM 和 65 μM。
T37924	7(Z)-Tricosene
	7(Z)-Tricosene is an unsaturated cuticular hydrocarbon that acts as a pheromone in some insects, including Drosophila. While it is present in both sexes of some Drosophila species, it is abundant in males, but not females, of D. melanogaster and D. sechellia. In these species, 7(Z)-tricosene prevents or reduces male courtship behavior and increases female sexual receptivity. It is absent from virgin D. melanogaster females, but is transferred from males to females during mating. In addition, mat...
T38279	C2-8 C2-8
	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...
T60661	CP681301
	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。
T71556	MK-1496
	MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a n...
T80251	Drosocin
	Drosocin为来自黑腹果蝇的具有生物活性的19聚体阳离子抗菌肽。其天然形态含有附着在链内苏氨酸残基上的二糖部分。相较之下，合成的Drosocin同样序列氨基酸构成但不包含二糖，显示出较原生天然化合物低的生物活性。
T36910	PF 04449913 maleate
	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:2...
T35993	Epitalon (acetate)
	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 melatoni...

化合物

Cat.No: T22026

Target: Others, Sirtuin

Cat.No: T6111

Synonym: EX-527,司来司他,SEN0014196

Target: Sirtuin

Cat.No: T68110

Antennapedia Peptide TFA(188842-14-0 free base)

Cat.No: TP1318

Synonym: Antennapedia Peptide(TFA)

Target: Others

Cat.No: T15775

Target: GABA Receptor, Parasite

Cat.No: T26684

Synonym: Auten-99,Auten-99 hydrochloride. Auten-99 HBr,Auten99,Auten 99

Target: Phosphatase

Chlorantraniliprole

Cat.No: T60127

Synonym: Rynaxypyr,Chlorantranilipole,Rynaxpyr

Target: Others

Cat.No: T41087

Neomyosuppressin

Cat.No: T25862

Synonym: Thr-asp-val-asp-his-val-phe-leu-arg-phenh2,Dromyosuppressin,Neb-MS

Cat.No: T28064

Synonym: ML 207,LLI01-022,ML-207

Cat.No: T80399

DL-Leucyl-DL-phenylalanine

Cat.No: T40644

Cat.No: T36801

7(Z),11(Z)-Pentacosadiene

Cat.No: T37922

Antennapedia Peptide

Cat.No: TP1840

7(Z)-Pentacosene

Cat.No: T37923

Ceramide Phosphoethanolamines (bovine)

Cat.No: T36188

C2 Ceramide (d14:1/2:0)

Cat.No: T36230

Synonym: C2 Ceramide (d14:1/2:0)

AD57 (hydrochloride)

Cat.No: T22552

Target: Others

Cat.No: T71552

6-Aminophenanthridine

Cat.No: T38187

Cat.No: T6664

Target: Apoptosis

Cat.No: T37924

Cat.No: T38279

Synonym: C2-8

Cat.No: T60661

Cat.No: T71556

Cat.No: T80251

PF 04449913 maleate

Cat.No: T36910

Epitalon (acetate)

Cat.No: T35993

Cat. No.	Product Name	Target	Signaling Pathways
T4136	Lapachol Bethabarra wood,CI75490,黄钟花醌,Greenhartin,Tecomin	Others; Influenza Virus; Antibacterial; Parasite; Antifungal	Microbiology/Virology; Others
	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。
TN1078	Seneciphylline 千里光菲灵碱,千里光非灵	P450; GST	Metabolism; oxidation-reduction
	Seneciphylline 是一种有毒的吡咯烷核生物碱，存在于千里光植物中。它显著增加了环氧水合酶和谷胱甘肽-S-转移酶的特性，但导致细胞色素 P-450 和相关单加氧酶特性的抑制。
T24175	Xanthumin
	Xanthumin is a naturally occurring insect development inhibitor against Drosophila melanogaster. Xanthumin is also an antibacterial compound.
TN5580	Rediocide A
	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
T36828	9(Z)-Tricosene
	(9Z)-Tricosene is a pheromone released by insects, including D. melanogaster, M. domestica (house fly), and A. mellifera L. (honey bee). In Drosophila, it induces aggregation behavior and is an oviposition guidance cue for females. Due to its aggregation-inducing activity, it is used as a bait pesticide to attract insects to traps. The mechanism of action in Drosophila is the activation of antennal basiconic Or7a receptors. It is also highly produced by honey bees during the waggle dance, which ...

天然产物

Cat.No: T4136

Synonym: Bethabarra wood,CI75490,黄钟花醌,Greenhartin,Tecomin

Target: Others, Influenza Virus, Antibacterial, Parasite, Antifungal

Cat.No: TN1078

Synonym: 千里光菲灵碱,千里光非灵

Target: P450, GST

Cat.No: T24175

Cat.No: TN5580

Cat.No: T36828

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