clathrin

Clathrin-IN-1 is a inhibitor of clathrin, and inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. It has the potential for anti-cancer research.

Clathrin-IN-25 is the most effective clathrin terminal domain-amphiphysin inhibitor reported to date.

Pitstop2 is an amphipathic protein-bound inhibitor of the clathrin terminal domain (IC50=12 μM) with selectivity. Pitstop2 severely interferes with receptor-mediated endocytosis, HIV entry and synaptic vesicle cycling. Pitstop2 has antitumor activity.

Ikarugamycin is a macrolide antibiotic discovered in Streptomyces, exhibiting antiprotozoal activity, inducing apoptosis and activating caspases, and also acting as a CME (clathrin-mediated endocytosis) inhibitor.

Clathrin-IN-1 is a selective clathrin inhibitor that acts by addressing clathrin function in cell physiology with potential applications as an inhibitor of virus and pathogen entry and as a modulator of cell signaling.

Hydroxy-Dynasore (Dyngo-4a) , a effective dynamin inhibitor, inhibits withDynI (brain), DynI (rec), and DynII (rec) of IC50 of 0.38 μM, 1.1 μM, and 2.3 μM, respectively.

Clathrin-IN-2 is a potent inhibitor of clathrin-mediated endocytosis (CME), demonstrating an IC50 value of 2.3 μM. Additionally, it exhibits inhibitory effects on dynamin I GTPase, with an IC50 of 7.7 μM.

Anti-Clathrin Heavy Chain Antibody is a highly specialized monoclonal antibody target and neutralize the clathrin heavy chain protein, inhibition of clathrin-mediated endocytosis by disrupting the formation of the polyhedral lattice structure across various cellular and molecular biology experimental models.

ES9-17, an analog of ES9 (endosidin9), is an inhibitor of clathrin-mediated endocytosis (CME). ES9-17 inhibits the uptake of FM4-64 and transferrin. ES9-17 inhibits root growth of Arabidopsis seedings.

Clathrin-IN-4 is an effective Clathrin inhibitor. It blocks endocytosis by disrupting clathrin assembly, used for studying viral entry mechanisms and receptor internalization.

Dynamin IN-2 (compound 43) is a Wiskostatin analogue. Dynamin IN-2 is a potent dynamin inhibitor (dynamin I GTPase, IC50= 1.0 μM). Dynamin IN-2 blocks clathrin mediated endocytosis (CME) (IC50= 9.5 μM).

Dynasore (Dynamin Inhibitor I) is a highly selective, reversible small-molecule dynamin inhibitor with an IC₅₀ of 15 μM. Dynasore also inhibits the mitochondrial dynamin Drp1 without affecting other small GTPases. By inhibiting the GTPase activity of dynamin, Dynasore blocks its function in membrane fission, thereby inhibiting clathrin-mediated endocytosis. Dynasore can be used in research on endocytosis, membrane transport, viral entry, and receptor signaling regulation.

IAV-IN-2 (Compound MC-22) inhibits influenza A virus (IAV) by preventing its entry into host cells via clathrin-mediated endocytosis (CME).

MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. It effectively reduces PD-L1 protein expression levels in various colorectal cancer (CRC) cell lines. The compound loses its ability to induce PD-L1 degradation upon HIP1R knockdown. MS1-96 binds directly to PD-L1 (KD= 2.58 μM) and enhances the interaction between HIP1R and PD-L1, altering PD-L1's intracellular transport in clathrin-coated vesicles. Additionally, MS1-96 induces abnormal N-glycosylation of PD-L1, leading to protein instability and accelerated lysosome-mediated degradation. MS1-96 is applicable for colorectal cancer research.

Pitstop 2d is a Clathrin inhibitor with an IC50 of less than 2 μM. It binds to the Clathrin N-terminal β-propeller domain, thereby inhibiting Clathrin's function and dynamics and blocking the entry of VSV. Pitstop 2d specifically inhibits clathrin-mediated endocytosis (Endocytosis) and does not interfere with non-clathrin-dependent endocytic processes.

Pitstop 2c is a Clathrin inhibitor with an IC50 of less than 2 μM. It binds to the Clathrin N-terminal β-propeller domain, impairing Clathrin's function and dynamics, and blocking the entry of vesicular stomatitis virus (VSV). Pitstop 2c inhibits clathrin-mediated endocytosis (Endocytosis) but does not inhibit non-clathrin-dependent endocytosis.

2H-Cho-Arg is a steroid-based cationic lipid that contains a 2H-cholesterol skeleton coupled to an L-arginine head group and can be used to facilitate gene transfection. It forms a complex with plasmid DNA (pDNA) and decreases pDNA migration in an electrophoretic mobility shift assay at +/- charge ratios of 4 or higher. 2H-Cho-Arg facilitates transfection of a luciferase gene into H1299 cells, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein , but not by inhibitors of clathrin- or micropinocytosis-mediated endocytosis. It induces cytotoxicity in H1299 cells (IC50 = 92.7 μg/ml).

Pitnot-2 is an inert analogue of the clathrin inhibitor Pitstop 2, commonly employed as a negative control in experimental studies.

Sulfonadyn-47 is a dynamin inhibitor that effectively inhibits dynamin GTPase activity with an IC50 of 3.5 µM in cell-free assays. Additionally, it disrupts clathrin-mediated endocytosis in U2OS cells (IC50 = 27.3 µM) and impedes the depolarization-stimulated uptake of the synaptic vesicle endocytosis (SVE) marker FM4-64 in isolated rat brain synaptosomes (IC50 = 12.3 µM). Significantly, in vivo administration of sulfonadyn-47 at doses of 30 and 60 mg/kg demonstrates anticonvulsant properties in the 6 Hz corneal kindling mouse model of seizures.

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

Rhodady C10 (Compound C10) functions as an inhibitor of dynamin I GTPase. It effectively blocks receptor-mediated endocytosis (IC50: 7 μM), a process involving dynamin in clathrin-independent endocytosis, phagocytosis, and caveolae internalization.

N-Sterol is a sterol lipid employed in the formation of lipid nanoparticles (LNP) for delivering mRNA both in vitro and in vivo. N-Sterol LNPs are absorbed by J774A.1 macrophages in a manner dependent on lipid composition, involving clathrin-coated pits, caveolin-mediated endocytosis, micropinocytosis, or phagocytosis at varying frequencies.