42
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9169 |
MPP+ iodide
|
Mitochondrial Metabolism; Autophagy | Autophagy; Metabolism |
MPP+ iodide 是一种 5-羟色胺转运体的高亲和力底物,也是一种神经毒素 MPTP 的有毒代谢物,通过选择性破坏黑质多巴胺能神经元,在动物模型中引起帕金森病症状。它被多巴胺转运体吸收进入多巴胺能神经元,通过影响呼吸链复合体 I 对线粒体发挥神经毒性作用。 | |||
T0239 |
Lonidamine
AF1890,氯尼达明,DICA,Diclondazolic Acid |
Apoptosis; Hexokinase; Mitochondrial Metabolism | Apoptosis; Metabolism |
Lonidamine (Diclondazolic Acid) 是一种抗肿瘤药物,是己糖激酶、线粒体丙酮酸载体和质膜单羧酸转运蛋白抑制剂,同时也抑制线粒体复合物 II。 | |||
T5337 |
IACS-010759
IACS-10759,IACS 10759,IACS10759 |
Apoptosis; Others; Mitochondrial Metabolism | Apoptosis; Metabolism; Others |
IACS-010759 是一种口服有效的线粒体氧化磷酸化复合物 I 抑制剂。它在依赖 OXPHOS 的脑癌和急性髓性白血病模型中抑制增殖并诱导细胞凋亡,有研究复发/难治性 AML 和实体瘤潜力。 | |||
T9714 |
Atpenin A5
|
Potassium Channel | Membrane transporter/Ion channel |
Atpenin A5 是高度特异性的complex II 抑制剂,IC50为 ~10 nM。Dolastatin 10也是有效的mKATP 通道激动剂,具有心脏保活的作用。 | |||
T4446 |
Tebufenpyrad
Pyranica,吡螨胺,MK239,Comanche |
Mitochondrial Metabolism | Metabolism |
Tebufenpyrad (Comanche) 是一种重要的农业化学杀螨剂,其作用类似于已知的线粒体毒物 rotenone。 | |||
T19714 |
Fenpyroximate
|
Others | Others |
Fenpyroximate 是一种有效的杀螨剂。 | |||
T9491 |
Pyraclostrobin
|
Antibacterial; Antifungal | Microbiology/Virology |
Pyraclostrobin 是一种球果苷杀菌剂,可诱导 3T3-L1 细胞内甘油三酯的积累,还可抑制真菌和哺乳动物细胞的线粒体复合物 III 。 | |||
T10404 |
ATP synthase inhibitor 1
|
ATPase | Membrane transporter/Ion channel |
ATP synthase inhibitor 1 是 F1/FO-ATP 合酶复合物 c 亚基的有效抑制剂,抑制线粒体通透性转换孔的开放。 | |||
T5114 |
Pyridaben
|
Calcium Channel; Parasite | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology |
Pyridaben 是一种METI 杀螨剂,可抑制复合物 I 处的线粒体电子转运。它对多种螨虫具有活性,通过滤纸接触给药,在 25 mg/mL、100 mg/mL 和 200 mg/mL 的剂量下,分别诱导 100% 的C. malaccensis,D. farina 和T. putrescentia 死亡率。 | |||
T14346 |
Aumitin
|
Others; Autophagy | Autophagy; Others |
Aumitin 是一种基于二氨基嘧啶的自噬抑制剂,以剂量依赖性抑制饥饿和雷帕霉素诱导的自噬,IC50分别为 0.12 μM 和 0.24 μM。它通过靶向复合物 I 抑制线粒体呼吸。 | |||
T36141 |
Boscalid
|
Mitochondrial Metabolism | Metabolism |
Boscalid 是一种广谱羧酰胺类杀菌剂,通过与线粒体复合物 II/琥珀酸脱氢酶的泛醌位点结合来抑制真菌呼吸。 | |||
T62238 |
AMPK activator 4
|
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
AMPK activator 4 是一种有效且具有选择性的AMPK激活剂,不抑制线粒体复合物 I。AMPK activator 4 选择性地激活肌肉组织中的 AMPK且剂量依赖性地改善正常小鼠的糖耐量,显著降低 db/db 糖尿病小鼠的空腹血糖水平和改善胰岛素抵抗。AMPK activator 4 具有降血糖作用。 | |||
T68508 | Ametoctradin | ||
Ametoctradin is a new Oomycete-specific fungicide and a potent Qo site inhibitor of the mitochondrial respiration complex III. | |||
T27516 | GW844520 | ||
GW844520 is a potent and selective inhibitor of the cytochrome bc1 complex of mitochondrial electron transport in P. falciparum. | |||
T34472 |
S1QEL
S-1QEL,S1 QEL,S 1QEL,S1QEL1.1,S1-QEL |
||
S1QEL is a suppressor of mitochondrial respiratory complex I site IQ electron leak which suppresses superoxide and/or H2O2 production without altering oxidative phosphorylation. | |||
T70032 |
NCI-006
|
||
NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition. | |||
T26573 |
AG311
AG 311,AG-311 |
||
AG311 is an inhibitor of complex I and hypoxia-induced HIF-1α stabilization. In vitro, AG311 induces rapid necrosis in numerous cancer cell lines. Within minutes, exposure to AG311 also results in mitochondrial depolarization, superoxide production, and i | |||
T70991 | Efrapeptin F | ||
Efrapeptin F is a metabolite of entomogenous fungi in the genus Tolypocladium that acts as a mitochondrial complex V inhibitor. It has been shown to express preferential cytotoxicity to nutrient-deprived tumor cells compared with nutrient-sufficient tumor cells. | |||
T79476 | SCAL-255 | Mitochondrial Metabolism | Metabolism |
SCAL-255,作为有效的线粒体复合物 I (CI) 抑制剂,具有 1.14 μM 的 IC50 值。该化合物通过抑制 OCR、诱导 ROS 产生并降低 MMP,干扰线粒体功能,对氧化磷酸化(OXPHOS)依赖性癌细胞显示出显著的抗增殖活性。 | |||
T37498 |
Antimycin A4
|
||
Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial elect... | |||
T26817 |
Bim-BLK-A
Bim Blocker A,Compound A,Bim BLK A,BimBLKA |
||
Bim-BLK-A efficiently blocks Bim-induced apoptosis after Bax is activated on the mitochondria. The cellular target of Bim-BLK-A was identified to be the succinate dehydrogenase subunit B (SDHB) protein of complex II of the mitochondrial electron transfer | |||
T36822 |
Benzovindiflupyr
|
||
Benzovindiflupyr is a fungicide.1It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH; IC50= 5.2 nM), and mycelial growth ofS. sclerotiorum(EC50= 0.011 μg/ml). Benzovindiflupyr (60 μg/ml) completely protects eggplant leaves fromS. sclerotioruminfection. Formulations containing benzovindiflupyr have been used to control various fungal diseases in agriculture. 1.Gao, Y., He, L., Zhu, J., et al.The relationship between features enabling SDHI fungicide binding to the Sc-S... | |||
T79477 | SCAL-266 | Mitochondrial Metabolism | Metabolism |
SCAL-266为线粒体复合物I (CI) 的有效抑制剂,IC50值为0.83 μM。它能够抑制线粒体功能,阻断氧耗量率(OCR),诱导活性氧(ROS)的产生,降低线粒体膜电位(MMP)。此外,SCAL-266对依赖氧化磷酸化(OXPHOS)的癌细胞展示出强烈的抗增殖效果。 | |||
T64311 | KUSC-5037 | ||
KUSC-5037 是一种 HIF-1 的有效抑制剂,其 IC50 值为 1.2 μM。KUSC-5037 对线粒体呼吸复合体 V 和 FoF1ATP 合酶表现出抑制作用。 | |||
T72199 | Antiproliferative agent-10 | ||
Antiproliferative agent-10 是一种抗肿瘤钌(II)-三吡唑基甲烷复合物,可通过抑制线粒体钙摄入抑制癌细胞的生长。 | |||
T37297 | Ru360 | ||
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce... | |||
T74921 | Antiproliferative agent-12 | ||
Antiproliferative agent-10 (compound 1) 是一种钌(II)-三吡唑基甲烷抗肿瘤复合物,能够通过阻断线粒体钙吸收来抑制癌细胞增殖。 | |||
T70957 |
NMac1
|
||
NMac1is a small molecule phenylbutenoid dimer that has novel anti-proliferative effect only under glucose starvation in metastatic breast cancer cells. NMac1 causes significant activation of AMPK by decreasing ATP synthesis, lowers mitochondrial membrane potential (MMP, ΔΨm), and inhibits oxygen consumption rate (OCR) under glucose starvation. These effects of NMac1 are provoked by a consequence of OXPHOS complex I inhibition. | |||
T83800 |
6-Biotin-17-NAD+ sodium
6-Biotin-17-Nicotinamide adenine dinucleotide,β-Nicotinamide-N6-(2-(6-(6-[biotinyl]aminohexanoyl)aminohexanoyl)aminoethyl)adenine dinucleotide |
||
6-Biotin-17-NAD+ 是信号分子及酶辅因子NAD+的生物素化衍生物,已应用于高通量筛选(HTS)中,用于测定线粒体复合物I(又称NADH脱氢酶)的活性。 | |||
T37469 |
Sitamaquine tosylate
|
||
Sitamaquine is an antileishmanial agent.1It is active againstL. donovani,L. infantum,L. mexicana,L. braziliensis, andL. tropica(EC50s = 9.5-19.8 μM). It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH), in a cell-free assay when used at concentrations ranging from 10 to 200 μM.2Sitamaquine (100 μM) increases intracellular levels of reactive oxygen species (ROS) and decreases intracellular ATP levels, as well as induces phosphatidylserine externalization, chromatin f... | |||
T79285 |
TRAP1-IN-1
|
HSP | Cytoskeletal Signaling; Metabolism |
TRAP1-IN-1(化合物35)是一种高效、具有高选择性的TRAP1抑制剂,其中TRAP1为Hsp90蛋白质家族中的一种线粒体同源体。该抑制剂对TRAP1的选择性优于Grp94超过250倍,能够破坏TRAP1四聚体的稳定性,并诱导下游蛋白质的降解。此外,TRAP1-IN-1能够抑制线粒体氧化磷酸化复合体(OXPHOS),破坏线粒体膜电位,并促进糖酵解过程。 | |||
T35712 |
Debutyldronedarone hydrochloride
SR35021 hydrochloride |
||
N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3’,5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide h... | |||
T36190 |
CAY10443
CAY10443 |
||
Mitochondrial release of cytochrome c triggers apoptosis via the assembly of a multimeric complex including caspase-9, Apaf-1, and other components, sometimes called the apoptosome. Library screens have identified small molecules that activate the apoptosome by binding to one or more of its components. CAY10443 is one such molecule. In a cell free, multi-component assay, it activated caspase-3 with an EC50 of 5 μM. These apoptotic activators represent therapeutic lead compounds for the developme... | |||
T78208 |
Leramistat
HMC-C-01-A,MBS2320 |
Mitochondrial Metabolism | Metabolism |
Leramistat (HMC-C-01-A; MBS2320)为线粒体复合物1抑制剂,关与调控细胞代谢及免疫代谢。该化合物被用于抑制诸如特应性皮炎的皮肤病、自身免疫性与炎症性疾病和癌症,以及破骨细胞介导的疾病。 | |||
T74680 | NecroIr1 | ||
NecroIr1 是一种铱 (III) 复合物,是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr1 选择性积累在线粒体中,导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr1 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL),调节CDK4表达。 | |||
T35552 |
Ganglioside GD3 Mixture (sodium salt)
|
||
Ganglioside GD3 is synthesized by the addition of two sialic acid residues to lactosylceramide and can serve as a precursor to the formation of more complex gangliosides by the action of glycosyl- and sialyltransferases. It induces apoptosis in HuT-78 cutaneous T cell lymphoma cells in a concentration-dependent manner and disrupts the mitochondrial membrane potential when used at a concentration of 200 μM. Expression of ganglioside GD3 in GD3-negative SK-MEL-28-N1 malignant melanoma cells increa... | |||
T74681 | NecroIr2 | ||
NecroIr2 是一种铱 (III) 复合物,是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr2 选择性积累在线粒体中,导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr2 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL),调节CDK4表达。 | |||
T36610 |
(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine
|
||
(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde ... | |||
T74501 | NHEJ inhibitor-1 | ||
NHEJ inhibitor-1 (Compound C2) 是一种三功能 Pt(II) 复合物,可缓解非同源末端连接 (NHEJ)/同源重组 (HR) 相关的双链断裂 (DSB) 修复,从而避免非小细胞肺对顺铂的耐药性。NHEJ inhibitor-1 抑制损伤修复蛋白 Ku70 和 Rad51,从而使肿瘤对活性分子重新敏感。NHEJ inhibitor-1 还诱导 ROS 产生和MMP 降低。 | |||
T79557 |
fac-[Re(CO)3(L6)(H2O)][NO3]
|
Apoptosis | Apoptosis |
fac-[Re(CO)3(L6)(H2O)][NO3](compound 6)是一种具有针对线粒体功能失调的抗癌活性的铼(I)三羰基水配合物。该化合物对前列腺癌细胞展现出显著的细胞毒性,具有50 nM的IC50值(PC-3细胞)。fac-[Re(CO)3(L6)(H2O)][NO3]能够主要集中在细胞核,抑制PC3细胞的ATP生成并诱导细胞凋亡,而不触发坏死、焦亡或自噬过程。 | |||
T79558 |
fac-[Re(CO)3(L3)(H2O)][NO3]
|
||
fac-[Re(CO)3(L3)(H2O)][NO3](简称compound 3),是一种与线粒体功能障碍相关的抗前列腺癌剂。这种铼(I)三羰基水配合物对前列腺癌细胞系(PC-3)表现出显著的细胞毒性,其IC50值为0.32 μM。研究表明,fac-[Re(CO)3(L3)(H2O)][NO3]主要在线粒体中积聚,能够降低PC-3细胞的ATP生成,进而触发细胞副凋亡(paraptosis)机制,而不通过引发坏死、凋亡或自噬途径作用。 | |||
T83865 |
HP661
|
||
HP661是一种针对线粒体复合物I(也称为NADH脱氢酶)的抑制剂,对复合物I具有选择性,以1 µM的浓度抑制其77.6%,而对复合物III抑制率为28.1%,对复合物II和IV则无抑制作用。HP661特异性降低具有高水平氧化磷酸化作用的人类肺癌细胞H460、NCI H441及对trametinib耐药的A549细胞的生存能力(IC50分别为10.6、29.7和15.1 nM),相较于氧化磷酸化水平低的NCI H358人类肺癌细胞(IC50 >10,000 nM)以及非癌性人类胰腺正常上皮细胞(HPNE)和MRC-5人类胎肺成纤维细胞(两者的IC50均>10,000 nM)。当以每天两次,每次30 mg/kg的剂量给药时,HP661在H460小鼠异种移植模型中减少肿瘤体积,并对trametinib引导的肿瘤生长减少产生加成效应。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8433 |
HQNO
|
Mitochondrial Metabolism | Metabolism |
HQNO 是一种电子传递链抑制剂,对 complex III 的Kd 值为 64 nM,由P. aeruginosa 产生的。它是许多物种的线粒体NDH-2的有效抑制剂。 | |||
T2970 |
Rotenone
Rotenon,鱼藤酮,Paraderil,Barbasco,Rotocide,Dactinol |
Apoptosis; Dehydrogenase; Mitochondrial Metabolism; p53; Autophagy | Apoptosis; Autophagy; Metabolism |
Rotenone (Rotocide) 属于天然产物,是一种植物杀虫剂。Rotenone 是一种线粒体电子传递复合物 I 抑制剂,可以促进线粒体产生活性氧,并诱导细胞凋亡。 | |||
T14293 |
Annonacin
|
Others | Others |
Annonacin is an Acetogenin and promotes cytotoxicity via a pathway inhibiting the mitochondrial complex and it is the active agent found in Graviola leaf extract to act as an inhibitor of sodium/potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pu | |||
T35667 |
Napyradiomycin A1
Napyradiomycin A1 |
||
Napyradiomycin A1is a fungal metabolite originally isolated fromC. rubraand has diverse biological activities.1,2It is active againstS. aureus,M. luteus,B. anthracis,C. bovis, andM. smegmatis(MICs = 1.56-12.5 μg/ml).1Napyradiomycin A1is an estrogen receptor antagonist (IC50= 4.2 μM in rat uterine homogenates).2It also inhibits mitochondrial NADH:ubiquinone oxidoreductase (complex I) and succinate:ubiquinone oxidoreductase (complex II) activities in bovine heart homogenates (IC50s = 20 and 9.7 μM... |