mitochondrial respiration

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) 是一种高度特异性的线粒体丙酮酸载体抑制剂，Ki<0.1 nM。它是一种线粒体呼吸抑制剂。它也能抑制质膜单羧酸转运体的 L-乳酸转运，但浓度比 MPC 的大 4 个数量级。

Mitochondrial respiration-IN-1 hydrobromide (compound 49) is a potent mitochondrial inhibitor (IC50=8.8 mg mL). Mitochondrial respiration-IN-1 hydrobromide significantly reduces mitochondrial respiration in platelets[1].

Mitochondrial respiration-IN-3 是 Dalfopristin 的氟衍生物。Mitochondrial respiration-IN-3 具有细胞膜渗透性。Mitochondrial respiration-IN-3 可以抑制胶质母细胞瘤干细胞的线粒体翻译 (mitochondrial translation)。Mitochondrial respiration-IN-3 可用于癌症的研究

Mitochondrial respiration-IN-2 是Virginiamycin M1 的氟衍生物。Mitochondrial respiration-IN-2 可以抑制胶质母细胞瘤干细胞的线粒体翻译。

Azoxystrobin (Bankit) 是一种广谱杀菌剂。 Azoxystrobin 通过阻断细胞色素 b 和 c1 之间的电子转移来诱导 ROS 产生、细胞凋亡和线粒体呼吸。

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。

(S)-Malic acid ((S)-2-Hydroxysuccinic acid) 是天然存在的二羧酸，是水果酸甜味的来源，常用作食品添加剂。

1-Hexanol (hexan-1-ol) 是一种伯醇，是一种表面活性剂，通过非质子机制解偶联线粒体呼吸，可用于增强工业过程中的界面性能。

CCI-006 是一种 MLL 重排白血病细胞的选择性抑制剂和化学增敏剂。 它能够抑制线粒体呼吸，造成 MLL-r 白血病细胞亚群中无法克服的线粒体去极化和促凋亡未折叠蛋白反应。

Z16078526 enhances thermogenesis in mice by inducing endogenous Ucp1 expression, promoting p38 MAPK phosphorylation, and stimulating lipolysis in primary mouse brown adipocytes. Additionally, it activates thermogenic gene expression and mitochondrial activity, specifically uncoupled respiration, in these cells.

Levocarnitine propionate (L-Propionylcarnitine) 是丙酰辅酶 A （Pro-CoA）衍生物，具有抗缺血功效，对 肌肉左旋肉碱转移酶 具有高亲和力。Levocarnitine propionate 增强糖尿病大鼠心脏中的底物氧化和线粒体呼吸，可使胃溃疡面积减少，诱导粘膜恢复，可用于研究急性呼吸窘迫综合征和阿尔茨海默病慢性胃溃疡。

Mito-apocynin (C11)是一种线粒体靶向抗氧化剂，通过靶向和中和细胞呼吸过程中产生的活性氧（ROS）发挥作用。三苯基溴化鏻已被发现能有效预防线粒体功能障碍，线粒体功能障碍是衰老过程和各种疾病的主要原因。它具有抗炎、抗凋亡和抗氧化活性。

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。

Trifluralin （Treflan） 是一种农用除草剂，具有轻微的毒性。Trifluralin 是一种新型污染物，可干扰线粒体呼吸。

LW1564 是一种 HIF-1α 抑制剂，在 HepG2 细胞中的 IC50 为 1.2 µM。它能够抑制线粒体呼吸，减少 ATP 生成，刺激 HIF-1α 降解，从而抑制多种癌细胞增殖，其 GI50 范围为 0.4-4.6 μM。LW1564 的作用机制还包括激活 AMPK 信号通路和抑制脂质合成。在 HepG2 异种移植小鼠模型中，LW1564 展示了抗肿瘤活性。

Dopaminechrome (DACHR) 是多巴胺的氧化产物，能在脑线粒体复合体 I 中促进 H2O2的生成，其过程依赖于浓度和呼吸。Dopaminechrome 具神经毒性特性，可用于帕金森病的研究。

SHO1122147 (Compound 7m) 通过影响线粒体电子传递链展现出线粒体解偶联活性（EC50=3.6 μM），提升细胞耗氧率（OCR=69%）并促进细胞呼吸。SHO1122147 具备口服活性，适用于肥胖和代谢功能障碍相关脂肪性肝炎 (MASH) 的研究。

6-Benzylthioinosine, a broad-spectrum metabolic inhibitor, inhibits glucose uptake, decreases glycolysis and ATP concentration with minimal changes in ROS and mitochondrial respiration.

Hexafluoro is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrates activity in Vemurafenib-resistant melanoma in vivo.

Honokiol DCA is an inhibitor of DRP1 phosphorylation. Honokiol DCA stimulates a phenotype suggestive of respiration through mitochondrial normalization and demonstrating activity in Vemurafenib-resistant melanoma in vivo.

Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.

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 electron transport chain (ETC). Antimycin A prevents the transfer of electrons between the b-cytochromes and ubiquinone at the Q(inner) site of complex III. This results in the stabilization of the ubisemiquinone radical at the Q(outer) site of complex III, leading to increased production of superoxide. Antimycin A is widely used in research to shunt electron flow through the ETC to study the chemical details of oxygen respiration. Additionally, antimycin A has been shown to inhibit Bcl-2 and Bcl-xL proteins, inducing apoptosis.

Piericidin B is a bacterial metabolite that has been found inS. mobaraensisand has insecticidal and antimicrobial activities.1,2,3It inhibits NADH oxidase activity in isolated bovine heart mitochondria and inhibits respiration in isolated rat liver mitochondria and isolated cockroach (P. americana) muscle mitochondria.2,3Topical application of piericidin B (4 μg insect) induces mortality in 87.5% of houseflies (M. domestica).1It induces 93.3, 100, and 100% mortality in rice stem borer (C. simples), silkworm (B. mori), and green caterpillar (P. rapae) larvae, respectively, when applied at respective concentrations of 60, 4.8, and 96 μg larva. Piericidin B is active against the fungiT. asteroides,T. rubrum,M. gypseum, andC. neoforms(MICs = 20, 10, 20, and 2 μg ml, respectively), as well as the bacteriaM. luteusandP. vulgaris(MICs = 50 and 100 μg ml, respectively). 1.Takahashi, N., Suzuki, A., Kimura, Y., et al.Isolation, structure and physiological activities of piericidin B, natural Insecticide produced by a StreptomycesAgr. Biol. Chem.32(9)1115-1122(1968) 2.Jeng, M., Hall, C., Crane, F.L., et al.Inhibition of mitochondrial electron transport by piericidin A and related compoundsBiochemistry7(4)1311-1322(1968) 3.Mitsui, T., Fukami, J.-I., Fukunaga, K., et al.Studies on piericidin. I. : Effects of piericidin A and B on mitochondrial electron transport in insect muscle comparing with rotenoneSci. Insect Control34(3)126-134(1969)

Picoxystrobin, a prominent primary strobilurin fungicide, is extensively utilized for efficient plant disease management. By obstructing electron transfer at the Qo center of cytochrome b and c1, picoxystrobin effectively halts mitochondrial respiration[1].