drp1

Drp1 peptide inhibitor P110（Compound P110）作为一种选择性Drp1肽抑制剂，显示出显著的神经保护效果。该化合物能有效抑制Drp1活性，阻止由MPTP诱导的Drp1线粒体定位改变，并有助于减轻由MPTP引起的多巴胺能神经元损失、神经末梢损伤及行为缺陷，适用于阿尔兹海默症研究。此外，Compound P110在治疗亨廷顿病、脑缺血损伤及心肌梗死动物模型中，也能显著减轻线粒体及器官损伤。

Drp1-IN-1 (comp A-7) 是一种 Drp1 蛋白抑制剂 (IC50: 0.91 μM)。

P110 TFA 是一种 dynamin-related protein 1 (Drp1) 抑制剂，抑制 Drp1 GTPase 活性。

DRP1i27是一种有效抑制人源Drp1(动力蛋白相关蛋白1)的化合物。它通过与Drp1的GTPase位点结合，并与Gln34及Asp218形成氢键来发挥作用。DRP1i27主要针对Drp1介导的线粒体裂变细胞系模型，能有效防止模拟缺血再灌注引起的损伤。

Mdivi-1 (Mitochondrial division inhibitor 1) 是一种线粒体分裂抑制剂，抑制 DRP1 和 Dynamin I (IC50=1-10 μM)。Mdivi-1 可以抑制线粒体自噬。

Anti-inflammatory agent 49 是一种高效的Drp1-Fis1相互作用的抑制剂，抑制 GTPase，可用于研究线粒体功能障碍引起的疾病。

Dynasore (Dynamin Inhibitor I) 是一种可渗透细胞的化学物质，可逆且非竞争性地抑制 dynamin 1 2 的 GTPase 活性。 它还抑制线粒体动力蛋白 Drp1，对其他小 GTPase 没有影响。

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) 是在多种中草药中发现的一种黄酮类天然产物。它抑制 TLR4 和 Myd88 表达，还降低 Drp1 表达和磷酸化，并减少线粒体分裂，具有抗氧化和抗癌活性。

Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-​1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.)​. Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mitochondrial fission, and improved right ventricular diastolic dysfunction during IR injury.

Dynamin-related protein 1 (Drp1) inhibitor, inhibits Drp1 GTPase activity. Displays no effect on dynamin 1 or other mitochondrial dynamics-related proteins. Inhibits mitochondrial fission, dysfunction and reactive oxygen species (ROS) production in vitro.

AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in H9c2 cells. AZT triphosphate accumulation causes downregulation of Opa1 and upregulation of Drp1. AZT triphosphate causes mitochondrial dysfunction, increases the production of cytotoxic reactive oxygen species (ROS), and impairs the balance of the mitochondrial quality control system in H9c2 cell model established from rat embryonic myoblasts[1]. [1]. Ryosuke Nomura, et al. Azidothymidine-triphosphate Impairs Mitochondrial Dynamics by Disrupting the Quality Control System. Redox Biol. 2017 Oct;13:407-417. [2]. Takeya Sato, et al. Engineered Human tmpk/AZT as a Novel Enzyme/Prodrug Axis for Suicide Gene Therapy. Mol Ther. 2007 May;15(5):962-70. [3]. K Y Hostetler, et al. Enhanced Oral Absorption and Antiviral Activity of 1-O-octadecyl-sn-glycero-3-phospho-acyclovir and Related Compounds in Hepatitis B Virus Infection, in Vitro. Biochem Pharmacol. 1997 Jun 15;53(12):1815-22.

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.

Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion. Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815

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.

POSH-IN-2 (MIDI) 作为一种DRP1抑制剂，能有效抑制细胞应激和遗传性线粒体损伤引起的线粒体分裂。该化合物通过与DRP1-C367共价结合，阻断DRP1与其多个受体的交互作用，从而实现其线粒体分裂抑制功能。

IIQLPEIVVV TFA 作为Drp1-Mff相互作用的特异性抑制剂，能够区分正常和病态的线粒体裂变，并且特别抑制正常裂变过程，进一步引发线粒体功能障碍。此化合物也被应用于研究亨廷顿氏病。