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38

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T83666 Kisspeptin-10 (zebrafish) TFA

Tyr-Asn-Leu-Asn-Ser-Phe-Gly-Leu-Arg-Tyr-NH2,Kp-10

Kisspeptin-10是一种在斑马鱼的大脑、卵巢和睾丸中表达的神经肽,参与性腺发育和类固醇表达。在10 ng/ml的浓度下使用时,能提高孤立的斑马鱼卵巢滤泡中编码黄体生成素(luteinizing hormone, Lh)受体,以及孕酮受体a (Progestin receptor a, Pra)和Prb的mRNA水平。在0.1和1 µg/g的剂量下给予时,Kisspeptin-10能在雌性金鱼中增加黄体生成素的血清水平,但在雄性金鱼中则不会。
T6759 AP-III-a4

ENOblock

Glucokinase Metabolism
AP-III-a4 (ENOblock) 是第一个非底物类似物,可直接与烯醇酶结合,IC50=0.576 uM,可阻碍体内癌细胞转移。
T16409 OSMI-1

Others; Acyltransferase Metabolism; Others
OSMI-1 是一种 O-GlcNAc 转移酶 (OGT) 抑制剂 (IC50=2.7 μM),具有口服活性和细胞渗透性。OSMI-1 可以抑制蛋白质 O-GlcNA 酰化,而不会定性地改变细胞表面 N- 或 O- 连接的聚糖。
T1348 Diphenyl phosphate

磷酸二苯酯,Phenyl hydrogen phosphate

Others Others
Diphenyl phosphate (Phenyl hydrogen phosphate) 能够性别特异性的抑制斑马鱼的生长和能量代谢。
T15273 Fedovapagon

VA483,A106483

Vasopressin Receptor GPCR/G Protein
Fedovapagon (VA106483) 是一种具有选择性和高效性的加压素 V2 受体 (V2R) 激动剂,可抑制斑马鱼节间血管的生长。Fedovapagon 可用于研究膀胱过度活动症、夜尿症和膀胱疼痛综合征。
T5095 Oxazolone

4-乙氧基亚甲基-2-苯基-2-唑啉-5-酮,4-Ethoxymethylene-2-phenyl-2-oxazolin-5-one

Others Others
Oxazolone 已被用作半抗原化剂,可在成年斑马鱼肠道组织中诱导炎症反应,并可用作两种形式的炎症性肠病(如克罗恩病和溃疡性结肠炎)的基因表达研究模型。
T60644 SJ000063181

TGF-beta/Smad Stem Cells
SJ000063181 是一种有效的BMP 信号激活剂,EC50≤1 μM。SJ000063181 可以作为化学探针来探索 BMP 信号,因为它可以穿透斑马鱼胚胎。
T8782 MitoBloCK-11 (MB-11)

Others Others
MitoBloCK-11 (MB-11) 是线粒体蛋白输入的小分子抑制剂,可能通过转运蛋白 Seo1 起作用,但不通过 Tom70 或 Tom20;抑制含有疏水片段的前体蛋白,以特定方式在缺乏尿嘧啶的培养基中促进生长,并影响斑马鱼的发育。
T76251L Ac-FEID-CMK TFA

Pyroptosis Apoptosis; Immunology/Inflammation
Ac-FEID-CMK TFA 是一种选择性斑马鱼 GSDMEb 衍生肽抑制剂,可减少感染性休克的死亡率和肾损伤。Ac-FEID-CMK TFA 在体内可抑制焦亡,缓解败血性 AKI (急性肾损伤),抑制 caspy2 介导的非典型炎症小体通路发挥作用。
T4687 Ro5-3335

CBFβ-Runx1 inhibitor II,Ro 5-3335

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Ro5-3335 (CBFβ-Runx1 inhibitor II) 是苯二氮化合物,是RUNX1-CBFβ 相互作用抑制剂,可抑制 RUNX1/CBFB 依赖性反式激活,能作为核心结合因子 (CBF) 白血病抑制剂。
T16696 Pyriproxyfen

S-31183,吡丙醚

Others Others
Pyriproxyfen (S-31183) 是昆虫生长调节剂,具有杀虫的作用, 属保幼激素类似物。
T30571 BPP

BPP is a fluorescent microviscosity probe used to image natural HOBr in living cells and zebrafish.
T36092 Fenobucarb

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.
T81828 MDYYFEER

MDYYFEER 是源自 C-藻蓝蛋白胰酶水解产物的抗氧化活性肽,能有效清除 DPPH 及 ABTS 自由基,并能保护斑马鱼幼虫免受 H2O2 诱导的氧化损害。
T78524 Polystyrene

Others Others
聚苯乙烯微塑料(PS-MPs)是一种潜在的有毒危害物质,对斑马鱼心脏造成损害,同时能诱导小鼠雄性生殖毒性。
T81800 MHLWAAK

MHLWAAK,抗氧化活性肽,源自C-藻蓝蛋白胰酶水解产物。该肽展现出显著DPPH及ABTS自由基清除效能,并能保护斑马鱼幼虫不受H2O2诱导的氧化损害。
T41179 CL 82198 hydrochloride

CL 82198 hydrochloride is a selective inhibitor of MMP-13 (89% inhibition at 10μg/mL) that displays no activity at MMP-1, MMP-9 or TACE. Inhibitsin vitroinvasion by the human pituitary adenoma cell line HP75. Rescues paclitaxel induced axon degradation and reduces associated neurotoxicity in zebrafish.
T68907 Flutolanil

Flutolanil is a benzanilide fungicide. It is active against a panel of 241 field isolates of the plant pathogenic fungus R. solani when grown in flutolanil-enriched growth media. Flutolanil inhibits R. solani hyphal growth and infection cushion formation on rice plant leaf sheaths. It is toxic to zebrafish embryos, larvae, and adults. Formulations containing flutolanil have been used to control fungal infections on rice crops.
T68790 Shinorine

Shinorine, a mycosporine-like amino acid (MAA), is a small molecule sunscreen produced in some bacteria. Shinorine ameliorates chromium induced toxicity in zebrafish hepatocytes through the facultative activation of Nrf2-Keap1-ARE pathway. Shinorine is also an analogue of porphyra-344. Both porphyra-334 and shinorine are antioxidants and direct antagonists of Keap1-Nrf2 binding. Shinorine may be a useful agent to prevent or retard the progression of multiple degenerative disorders of ageing. S...
T81827 MDYYFEER TFA

MDYYFEER TFA为从C-藻蓝蛋白胰酶水解产物中提取的抗氧化活性肽,展现了显著的DPPH与ABTS自由基清除效果,并能保护斑马鱼幼虫免遭H2O2诱导的氧化伤害。
T61072 ERD03

ERD03 是EXOSC3–RNA 相互作用的强效破坏剂,其Kd 值为 17±7 μM。ERD03 诱导斑马鱼胚胎 PCH1B 样表型,可用于脑神经失调的研究。
T81799 MHLWAAK TFA

MHLWAAK TFA是从C-藻蓝蛋白胰酶水解产物中分离的抗氧化活性肽。它展现出了较强的DPPH和ABTS自由基清除效应,并且能保护斑马鱼幼虫免遭H2O2引发的氧化伤害。
T81864 MAQAAEYYR

MAQAAEYYR 是从C-藻蓝蛋白的胰酶水解产物中分离得到的一种具备显著抗氧化活性的肽。它在DPPH和ABTS自由基清除实验中显示出较高的效率,并能有效保护斑马鱼幼虫免遭H2O2诱导的氧化伤害。
T79293 EGFR-IN-79

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
EGFR-IN-79(即化合物21)是抑制EGFR活性的抗肿瘤剂。该化合物能引发ROS依赖的细胞凋亡和EGFR/AKT/mTOR途径驱动的自噬,同时诱导EJ28球体增殖区与静止区的细胞死亡。在斑马鱼模型中,EGFR-IN-79显示了良好的安全性。
T76251 Ac-FEID-CMK

Ac-FEID-CMK 是一种有效的斑马鱼特异性GSDMEb 衍生肽抑制剂。Ac-FEID-CMK 可减轻感染性休克的死亡率和肾损伤。Ac-FEID-CMK 在体内可抑制焦亡,减轻败血性 AKI (急性肾损伤)。Ac-FEID-CMK 可抑制 caspy2 介导的非典型炎症小体通路。
T81863 MAQAAEYYR TFA

MAQAAEYYR TFA 是从 C-藻蓝蛋白胰酶水解产物中分离得到的一种具有高抗氧化活性的肽。它展现了显著的 DPPH 及 ABTS 自由基清除作用,并能有效保护斑马鱼幼虫不受 H2O2 诱导的氧化损伤。
T74745 A031

A031 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂,对 AR 蛋白具有降解作用,IC50值小于 0.25 μM。A031 抑制移植人前列腺癌 (VCaP) 的斑马鱼的肿瘤生长。
T83357 3-Hydroxy-2-(palmitoyloxy)propyl stearat

3-Hydroxy-2-(palmitoyloxy)propyl stearate是一种从棕色巨藻Fucus virsoides J. Agardh的极性较小部分分离得到的非挥发性化合物。该化合物具有良好的自由基清除能力,并能保护斑马鱼胚胎免受过氧化氢诱导的氧化应激。
T82771 CB2-H

CB2-H为一种高特异性双通道荧光探针,专门设计用于HOCl和ONOO-的同时检测。该探针在两个分离的通道中对HOCl和ONOO-无交叉干扰的检测能力使其适用于对活细胞和斑马鱼样本内HOCl及ONOO-的内源性水平进行双通道荧光成像分析,即使在不同生物刺激下也能保持准确性。
T74627 Angiogenesis inhibitor 3

Angiogenesis inhibitor 3 (compound 8) 是一种有效的血管生成(angiogenesis)抑制剂,能够抑制HUVEC和HCT-15细胞增殖,其IC50值分别为1.00和0.71 μM。此外,此化合物还能诱导这两种细胞的凋亡(apoptosis)并具有抑制癌细胞侵袭的抗癌活性。Angiogenesis inhibitor 3还能够抑制斑马鱼胚胎的血管生成。
T82357 GABA receptor Antagonist 1

GABA Receptor Membrane transporter/Ion channel; Neuroscience
GABA receptorAntagonist 1 (compound 7w) 在抑制PxRDL1GABAR方面具有高特异性,IC50为7.08 nmol/L。针对P. xylostella、S. frugiperda、S. exigua和S. litura的杀虫活性显著,相应的LC50值分别为0.09、0.84、0.87和0.68 mg/L。此化合物对蜜蜂的急性毒性为中等(48小时,LD50=2.22μg/成虫),而对斑马鱼的急性毒性较低(LC50: 42.4mg/L)。
T81154 SIRT1 activator 1

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
SIRT1 activator1(compound 3),作为海洋化合物xyloallenoide a的衍生物,最初从红树林真菌Xylaria sp中分离获得。该化合物在斑马鱼模型中展现了促进血管生成的活性,并且能够通过提升SIRT1的表达水平以及调节AMPK/Akt信号通路,来防护人类内皮祖细胞(hEPC)免受血管老化的影响。
T83068 Antifungal agent 77

Antifungalagent 77 (Compound 13h) 作为一种化合物,展现出对粘虫、棉铃虫、玉米螟及草地贪夜蛾的杀虫效力,其浓度为500 μg/mL时,相应的死亡率为30%、25%、40% 和 25%。同时,该化合物对斑马鱼胚胎具有毒性,其半致死浓度(LC50)为2.43 μg/mL。
T82635 Cy-FBP/SBPase-IN-1

Cy-FBP/SBPase-IN-1(compound S5)是一种针对蓝藻光合作用调节酶的Cy-FBP/SBPase抑制剂。该化合物能有效阻断卡尔文循环和光系统,从而减少蓝藻的光合效率。此外,Cy-FBP/SBPase-IN-1能抑制包括集胞藻PCC6803在内的蓝藻生长,并在人源细胞与斑马鱼模型中表现出良好的安全性。
T83771 6-PPD

Antioxidant 4020,N-(1,3-Dimethylbutyl)-N′-phenyl-p-phenylenediamine

6-PPD是一种取代的p-苯二胺。它通过形成亚硝基自由基来清除臭氧。当6-PPD的浓度分别为0.022 mg/L和0.22 mg/L时,斑马鱼胚胎的孵化能力分别下降了25.6%和78.9%。6-PPD还会降低斑马鱼胚胎的活动能力和体长,并诱导发育畸形及氧化应激。含有6-PPD的配方已作为橡胶中的稳定剂添加物和抗臭氧剂使用。
T35687 Collismycin A

Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs = 6.25 and 100 μg/ml) and fungi (MICs = 12.5-100 μg/ml). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s = 0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50 = 56.6 μM) but not MDA-MD-231 breast canc...
T37094 (S)-UFR2709 hydrochloride

(S)-UFR2709 hydrochloride

(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction[1][2]. Brain nicotinic acetylcholine receptors (nAChRs) is a heterogeneous family of pentameric acetylcholine-gated cation channels, whi...
T83721 Hexafluoropropylene Oxide Dimer Acid

FRD-903,Perfluoro-2-propoxypropanoic Acid,PFPrOPrA,HFPO-DA

Hexafluoropropylene oxide dimer acid (HFPO-DA)作为一种全氟烷基醚羧酸(PFECA),于HepG2细胞中以250 µM的浓度使用时,可诱导凋亡并增加活性氧种类(ROS)的水平。HFPO-DA以每个蛋4 mg/kg的剂量,会减少孵化鸡右心室壁厚度,增加心率,并诱导肝脏脂肪积累,这些效应可通过敲除过氧化物酶体增殖物激活受体α(Ppara)基因编码实现预防。它减少了斑马鱼胚胎的存活百分比(LC50 = 7,651 mg/L)。在孕妇大鼠给药下,HFPO-DA(250 mg/kg)降低了新生大鼠的平均出生体重、存活时间和血清葡萄糖水平,并增加了血清胆固醇和甘油三酯水平。它已经被发现污染海水和河水。

化合物

Kisspeptin-10 (zebrafish) TFA
Cat.No: T83666
Synonym: Tyr-Asn-Leu-Asn-Ser-Phe-Gly-Leu-Arg-Tyr-NH2,Kp-10
Target:
AP-III-a4
Cat.No: T6759
Synonym: ENOblock
Target: Glucokinase
OSMI-1
Cat.No: T16409
Synonym:
Target: Others, Acyltransferase
Diphenyl phosphate
Cat.No: T1348
Synonym: 磷酸二苯酯,Phenyl hydrogen phosphate
Target: Others
Fedovapagon
Cat.No: T15273
Synonym: VA483,A106483
Target: Vasopressin Receptor
Oxazolone
Cat.No: T5095
Synonym: 4-乙氧基亚甲基-2-苯基-2-唑啉-5-酮,4-Ethoxymethylene-2-phenyl-2-oxazolin-5-one
Target: Others
SJ000063181
Cat.No: T60644
Synonym:
Target: TGF-beta/Smad
MitoBloCK-11 (MB-11)
Cat.No: T8782
Synonym:
Target: Others
Ac-FEID-CMK TFA
Cat.No: T76251L
Synonym:
Target: Pyroptosis
Ro5-3335
Cat.No: T4687
Synonym: CBFβ-Runx1 inhibitor II,Ro 5-3335
Target: DNA/RNA Synthesis
Pyriproxyfen
Cat.No: T16696
Synonym: S-31183,吡丙醚
Target: Others
BPP
Cat.No: T30571
Synonym:
Target:
Fenobucarb
Cat.No: T36092
Synonym:
Target:
MDYYFEER
Cat.No: T81828
Synonym:
Target:
Polystyrene
Cat.No: T78524
Synonym:
Target: Others
MHLWAAK
Cat.No: T81800
Synonym:
Target:
CL 82198 hydrochloride
Cat.No: T41179
Synonym:
Target:
Flutolanil
Cat.No: T68907
Synonym:
Target:
Shinorine
Cat.No: T68790
Synonym:
Target:
MDYYFEER TFA
Cat.No: T81827
Synonym:
Target:
ERD03
Cat.No: T61072
Synonym:
Target:
MHLWAAK TFA
Cat.No: T81799
Synonym:
Target:
MAQAAEYYR
Cat.No: T81864
Synonym:
Target:
EGFR-IN-79
Cat.No: T79293
Synonym:
Target: EGFR
Ac-FEID-CMK
Cat.No: T76251
Synonym:
Target:
MAQAAEYYR TFA
Cat.No: T81863
Synonym:
Target:
A031
Cat.No: T74745
Synonym:
Target:
3-Hydroxy-2-(palmitoyloxy)propyl stearat
Cat.No: T83357
Synonym:
Target:
CB2-H
Cat.No: T82771
Synonym:
Target:
Angiogenesis inhibitor 3
Cat.No: T74627
Synonym:
Target:
GABA receptor Antagonist 1
Cat.No: T82357
Synonym:
Target: GABA Receptor
SIRT1 activator 1
Cat.No: T81154
Synonym:
Target: Sirtuin
Antifungal agent 77
Cat.No: T83068
Synonym:
Target:
Cy-FBP/SBPase-IN-1
Cat.No: T82635
Synonym:
Target:
6-PPD
Cat.No: T83771
Synonym: Antioxidant 4020,N-(1,3-Dimethylbutyl)-N′-phenyl-p-phenylenediamine
Target:
Collismycin A
Cat.No: T35687
Synonym:
Target:
(S)-UFR2709 hydrochloride
Cat.No: T37094
Synonym: (S)-UFR2709 hydrochloride
Target:
Hexafluoropropylene Oxide Dimer Acid
Cat.No: T83721
Synonym: FRD-903,Perfluoro-2-propoxypropanoic Acid,PFPrOPrA,HFPO-DA
Target:
Cat. No. Product Name Target Signaling Pathways
TN2296 Vinaginsenoside R4

越南参皂苷R4

Others Others
Vinaginsenoside R4 是分离自水培人参的叶子中。它能够抑制黑色素的生物合成,并增强斑马鱼的色素沉着,对 melan-a 细胞没有任何细胞毒性作用。
TMS1461 Qingyangshengenin B

青阳参甙元B,青阳参苷元B,Otophylloside B

Beta Amyloid Neuroscience
Qingyangshengenin B (Otophylloside B) 是一种分离自 Qingyangshen 的 C-21 甾体苷。它能够在 mRNA 水平上抑制 Aβ 的表达来减少 Aβ 的沉积,对 Aβ 的毒性有保护作用。它具有抗癫痫作用。
TCS2170 2,5-Dihydroxyacetophenone

Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 ',5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP

ERK; NF-κB; Tyrosinase MAPK; NF-κB; Proteases/Proteasome
2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物,通过阻断 ERK1/2和 NF-κB 信号通路,抑制活化巨噬细胞中炎症介质的产生。
TN4722 Otophylloside F

Others Others
Otophylloside F can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.
T38097 Antibiotic PF 1052

Antibiotic PF 1052 is a fungal metabolite originally isolated from Phoma.1,2 It is active against S. aureus, S. parvulus, and C. perfringens (MICs = 3.13, 0.78, and 0.39 μg/ml, respectively), among others.1 It inhibits neutrophil migration in a wound assay using zebrafish larvae expressing GFP-labeled neutrophils, reducing pseudopodia formation and inducing rounding of neutrophils.2 Antibiotic PF 1052 is selective for neutrophil migration over macrophage migration in zebrafish larvae. It also in...
T73069 Kurzipene D

Kurzipene D是一种有效的抗癌剂(anticanceragent),通过诱导HepG2细胞凋亡(apoptosis)并使其在S期阻滞,显示出明显的抗肿瘤作用。通过体内斑马鱼模型,Kurzipene D展现了其抑制肿瘤增殖和迁移的特性。
T75554 6-O-Isobutyrylbritannilactone

6-O-Isobutyrylbritannilactone 是一种天然的黑素生成抑制剂。6-O-Isobutyrylbritannilactone 是一种倍半萜,可从英菊花中分离得到。6-O-Isobutyrylbritannilactone 抑制 IBMX 诱导 B16F10 细胞产生黑色素。6-O-Isobutyrylbritannilactone 也调控 ERK、PI3K/AKT 和 CREB,在斑马鱼胚胎模型中显示出抗黑色素原活性。

天然产物

Vinaginsenoside R4
Cat.No: TN2296
Synonym: 越南参皂苷R4
Target: Others
Qingyangshengenin B
Cat.No: TMS1461
Synonym: 青阳参甙元B,青阳参苷元B,Otophylloside B
Target: Beta Amyloid
2,5-Dihydroxyacetophenone
Cat.No: TCS2170
Synonym: Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 ',5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP
Target: ERK, NF-κB, Tyrosinase
Otophylloside F
Cat.No: TN4722
Synonym:
Target: Others
Antibiotic PF 1052
Cat.No: T38097
Synonym:
Target:
Kurzipene D
Cat.No: T73069
Synonym:
Target:
6-O-Isobutyrylbritannilactone
Cat.No: T75554
Synonym:
Target:
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