Dynamin Inhibitor

P259 is a Drp1-Mff inhibitor. P259 distinguishes physiological from pathological fission by specifically inhibiting Drp1-Mff interaction. P259 elongates cell mitochondria and disrupts mitochondrial function and motility. P259 reduces ATP levels and alters mitochondrial structure in the brain, resulting in behavioral deficits in wild-type mice and a short lifespan in Huntington's disease (HD) mice model.

Drp1-IN-1 is a dynamin-1-like protein (Drp1) inhibitor with an IC₅₀ of 0.91 μM. Drp1 mediates the fission of the outer mitochondrial membrane. Drp1-IN-1 can be used to study diseases associated with mitochondrial dysfunction.

DynaMin inhibitory peptide, myristoylated is a DynaMin inhibitor to interfere with the binding of amphiphysin with dynamin. DynaMin inhibitory peptide, myristoylated is a membrane-permeant form of the peptide that prevents endocytosis.

Dynamin IN-1 is a potent dynamin inhibitor with an IC₅₀ value of 1.0 µM.

Drp1 peptide inhibitor P110 (Compound P110) is a selective Drp1 peptide inhibitor with neuroprotective properties. Drp1 peptide inhibitor P110 can inhibit the activation of Drp1, prevent MPTP-induced Drp1 mitochondrial translocation, and alleviate MPTP-induced dopaminergic neuron loss, dopaminergic nerve terminal damage, and behavioral deficits, and can be used in the study of Alzheimer's disease. Additionally, Drp1 peptide inhibitor P110 can reduce mitochondrial damage and organ injury in animal models of Huntington's disease, cerebral ischemic injury, and myocardial infarction.

Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors.

Trimethyloctadecylammonium bromide is an inhibitor of dynamin, with an IC₅₀ value of 1.9 μM for dynamin I. Trimethyloctadecylammonium bromide exhibits antibacterial activity against Staphylococcus aureus.

Drp1 peptide inhibitor P110 (Compound P110) TFA is a selective Drp1 peptide inhibitor with neuroprotective properties. Drp1 peptide inhibitor P110 TFA can inhibit the activation of Drp1, prevent MPTP (HY-15608)-induced Drp1 mitochondrial translocation, and alleviate MPTP-induced dopaminergic neuron loss, dopaminergic nerve terminal damage, and behavioral deficits, and can be used in the study of Alzheimer's disease. Additionally, Drp1 peptide inhibitor P110 TFA can reduce mitochondrial damage and organ injury in animal models of Huntington's disease, cerebral ischemic injury, and myocardial infarction.

Clathrin-IN-2 is potent inhibitor of clathrin mediated endocytosis (CME) with an IC₅₀ value of 2.3 μM. Clathrin-IN-2 also has inhibitiory for dyn I GTPase with an IC₅₀ value of 7.7 μM.

Dynamin IN-2 (compound 43), a Wiskostatin (HY-12534) analogue, is a potent dynamin inhibitor, with an IC₅₀ of 1.0 μM for dynamin I GTPase. Dynamin IN-2 also blocks clathrin mediated endocytosis (CME), with an IC₅₀ of 9.5 μM.

Bleomycin A5 (Pingyangmycin) hydrochloride is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 hydrochloride exerts cytotoxic effects by binding to Fe²⁺ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 hydrochloride inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 hydrochloride can be used in cancer research.

Sulfonadyn-47 is a GTP-competitive dynamin I (dynI) inhibitor that targets the active site in the GTPase domain of dynamin I, with IC₅₀ values of 3.5 μM against dynI, 27.3 μM in clathrin-mediated endocytosis (CME) assays, and 12.3 μM in synaptic vesicle endocytosis (SVE) assays. Sulfonadyn-47 increases seizure threshold. Sulfonadyn-47 can be used the study for the seizure.

DRP1 Allosteric-IN-3 (Compound 2b) is an allosteric inhibitor of DRP1. Its IC₅₀ value for the DRP1:MiD49 protein-protein interaction is 11 μM. DRP1 Allosteric-IN-3 can be used to study various diseases related to mitochondrial division disorders.

MB-0223 is a potent and selective dynamin-related GTPase Drp1 partial inhibitor (IC₅₀=1.3 μM) over other dynamin family members, Opa 1 and dynamin-1 (IC₅₀>100 μM).

DRP1 Allosteric-IN-2 (Compound 2a) is an allosteric inhibitor of DRP1. Its IC₅₀ value for the DRP1:MiD49 protein-protein interaction is 4.3 μM. DRP1 Allosteric-IN-2 can be used to study various diseases related to mitochondrial division disorders.

Clathrin-IN-3 (Compound 25) is a Clathrin inhibitor (IC₅₀: 6.9 μM). Clathrin-IN-3 potenly inhibits clathrin terminal domain-amphiphysin PPI.

DynaMin inhibitory peptide, myristoylated TFA is a DynaMin inhibitor to interfere with the binding of amphiphysin with dynamin. DynaMin inhibitory peptide, myristoylated TFA is a membrane-permeant form of the peptide that prevents endocytosis.

DRP1 Allosteric-IN-1 (Compound 1) is an allosteric inhibitor of DRP1 with an IC₅₀ value for the DRP1:MiD49 protein-protein interaction of 3.6 μM. DRP1 Allosteric-IN-1 can be used to study various diseases related to mitochondrial division disorders.

Pyrimidyn 7 is an inhibitor of dynamin I/II with IC₅₀ values of 1.1 μM and 1.8 μM, respectively. Pyrimidyn 7 competitively inhibits the interactions between GTP and phospholipids with dynamin I. Additionally, Pyrimidyn 7 reversibly inhibits clathrin-mediated endocytosis (CME) of transferrin and epidermal growth factor (EGF) in various non-neuronal cell linecell^[1.

N,N-Dimethyldodecylamine is a dynamin I inhibitor. N,N-Dimethyldodecylamine has an IC₅₀ value of 14.79 μM for GTPase activity of dynamin I. N,N-Dimethyldodecylamine can be used in the research of diseases associated with endocytic defects, such as Alzheimer's disease and Huntington's disease.