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Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. Pitstop 2 has the potential for anti-cancer research .
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 .
TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity .
Clathrin-IN-1 is a selective clathrin-mediated endocytosis (CME) inhibitor. Clathrin-IN-1 selectively inhibits amphiphysin association of clathrin terminal domain (TD) with an IC50 value of 12 μM. Clathrin-IN-1 acutely interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling .
Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis . CME: Clathrin mediated endocytosis
Clathrin-IN-4 (compound 8b), a Wiskostatin (HY-12534) analogue, is a potent inhibitor of clathrin mediated endocytosis with an IC50 of 2.1 μM. Clathrin-IN-4 is a dynamin I GTPase activity inhibitor with an IC50 of 9.1 μM .
Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
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 .
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of AMPAR. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression .
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .
Clemastanin B, a lignin, has potent anti-influenza activities by inhibiting the virus multiplication, prophylaxsis and blocking the virus attachment. Clemastanin B targets viral endocytosis, uncoating or ribonucleoprotein (RNP) export from the nucleus. Clemastanin B has antioxidant and anti-inflammatory activities .
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
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 .
Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
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 .
IAV-IN-2 (Compound MC-22) inhibits for Influenza A Virus (IAV) through blocking the entry of IAV into host cell via clathrin-mediated endocytosis (CME) .
Arg-Flipper 34 is one of the flipper probes which have been introduced as small molecule fluorophores to image membrane tension in living systems. Arg-Flipper 34 can be used to assess the mechanics of early endocytosis .
4-Sulfo-N-(4-aminobenzyl)-1,8-naphthalimide potassium is an inactive 1,8-Naphthalimide derivative. 4-Sulfo-N-(4-aminobenzyl)-1,8-naphthalimide potassium can be used as a negative control for the clathrin inhibitor 3-Sulfo-N-benzyl-1,8-naphthalimide, potassium salt .
Biotin-TAT (47-57), a biotin tagged TAT, is a transactivator of transcription. Biotin-TAT (47-57) is one of the most widely used protein transduction domains (PTDs) into different primary cells is ATP- and temperature-dependent, indicating the involvement of endocytosis .
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .
Tat-GluR23Y, scrambled is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .
Tat-GluR23Y, scrambled TFA is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .
mPEG-amine (MW 350) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 550) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 750) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 3400) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively .
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
mPEG-amine (MW 4000) can be used to synthesize folate-conjugated polymer micelles for encapsulating anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
Fucosyltransferase 8 (EC:2.4.1.68; FUT8; α1-6FucT) is a glycosyl transferase and catalyzes the transfer of a fucose residue from GDP-fucose to the innermost N-acetylglucosamine residue of N-glycans .
Tafolecimab (IBI-306) is a human lgG2 monoclonal antibody that specifically binds PCSK-9 and reduces LDL-C levels by inhibiting PCSK-9-mediated endocytosis of the LDL receptor, which in turn enhances clearance of LDL-C and leads to a reduction in LDL-C levels. Tafolecimab may be used in studies of hypercholesterolaemia .
PEG-bis-amine (MW 8000) synthesizes folate-conjugated polymeric micelles for encapsulation of the anticancer agent 9-nitrocamptothecin HY-16560 (HY-16560). Folic acid-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
PEG-bis-amine (MW 1000) synthesizes folate-conjugated polymeric micelles for encapsulation of the anticancer agent 9-nitrocamptothecin HY-16560 (HY-16560). Folic acid-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) is a cyclic heptasaccharide used to deliver hydrophobic agents based on its property of solubilizing non-polar substances. Methyl-β-cyclodextrin is also extensively used as a cholesterol-depleting reagent . Methyl-β-cyclodextrin strongly reduces clathrin-dependent endocytosis . Methyl-β-cyclodextrin blocks cell migrasome formation .
4-Di-1-ASP is a styryl dye used to stain glioma cells in living brain tissue for analysis of cell structure, viability, proliferation and endocytosis, cytokinesis and phagocytosis, as well as for observation of mitochondrial structures in living cells. 4-Di-1-ASP fluoresces green when imaged microscopically (λex /λem = 475/606 nm) .
FM1-43 is a very lipophilic, water-soluble styrene dyes, can specifically bind to cell membranes and inner membrane organelles to produce fluorescence. FM1-43 is widely used in endocytic and exospic membrane structure markers.
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage . Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME) .
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
Pentabromophenol (PBP) is a brominated flame retardant (BFR) widely used in various consumer products to reduce the flammability of materials used in different utility items. Pentabromophenol can accelerate the degradation of transforming growth factor-β (TGF-β) receptors by promoting clathrin-mediated endocytosis, thereby inhibiting the TGF-β signaling pathway. Additionally, Pentabromophenol can also induce apoptosis in peripheral blood mononuclear cells (PBMCs) .
ES9-17 is an analog of ES9 (endosidin9), which is an inhibitor of clathrin heavy chain (CHC). ES9-17 is an inhibitor of clathrin-mediated endocytosis (CME), a major route for internalization of plasma membrane proteins and molecules from the extracellular environment in plants. ES9-17 inhibits the uptake of transferrin and FM4-64. ES9-17 also inhibits root growth of Arabidopsis seedings .
Phosphatidylserine is a conserved anti-inflammatory and immunosuppressive signal that is highly dysregulated in the tumor microenvironment and autoimmune diseases. During apoptosis and cellular stress，the related disrupting enzymes Xkr8 and TMEM16 mediate Phosphatidylserine externalization. Phosphatidylserine externalization produces a "eat me" signal that initiates endocytosis and helps clear the body of apoptotic cells. When pathogens use Phosphatidylserine and apoptotic mimicry to evade host immune responses，targeting Phosphatidylserine strategies can stimulate immune activity .
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
FM4-64 is a very lipophilic, water-soluble styrene dyes, can specifically bind to cell membranes and inner membrane organelles to produce fluorescence. FM4-64 is widely used in endocytic and exospic membrane structure markers.
Mipomersen sodium (ISIS 301012) is an antisense oligonucleotide inhibitor of apolipoprotein B (apoB). Mipomersen has anti-HCV effect and reduces the infectivity of the HCV. Mipomersen sodium can be used for the research of homozygous familial hypercholesterolemia (HoFH) .
Photosensitizer-2 (compound 1) is a organic D-π-A sensitizer against phototoxicity. Photosensitizer-2 contains an acrylic acid moiety that exerts high levels of phototoxicity. Photosensitizer-2 shows antitumor activity against HeLa cells, with IC50 values of 20.9 ± 4.5 μM (dark) and 0.046 ± 0.012 μM (irradiation), respectively .
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
4-Di-1-ASP is a styryl dye used to stain glioma cells in living brain tissue for analysis of cell structure, viability, proliferation and endocytosis, cytokinesis and phagocytosis, as well as for observation of mitochondrial structures in living cells. 4-Di-1-ASP fluoresces green when imaged microscopically (λex /λem = 475/606 nm) .
FM1-43 is a very lipophilic, water-soluble styrene dyes, can specifically bind to cell membranes and inner membrane organelles to produce fluorescence. FM1-43 is widely used in endocytic and exospic membrane structure markers.
Arg-Flipper 34 is one of the flipper probes which have been introduced as small molecule fluorophores to image membrane tension in living systems. Arg-Flipper 34 can be used to assess the mechanics of early endocytosis .
FM4-64 is a very lipophilic, water-soluble styrene dyes, can specifically bind to cell membranes and inner membrane organelles to produce fluorescence. FM4-64 is widely used in endocytic and exospic membrane structure markers.
mPEG-amine (MW 350) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 550) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 750) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 3400) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
mPEG-amine (MW 4000) can be used to synthesize folate-conjugated polymer micelles for encapsulating anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
Fucosyltransferase 8 (EC:2.4.1.68; FUT8; α1-6FucT) is a glycosyl transferase and catalyzes the transfer of a fucose residue from GDP-fucose to the innermost N-acetylglucosamine residue of N-glycans .
PEG-bis-amine (MW 8000) synthesizes folate-conjugated polymeric micelles for encapsulation of the anticancer agent 9-nitrocamptothecin HY-16560 (HY-16560). Folic acid-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
PEG-bis-amine (MW 1000) synthesizes folate-conjugated polymeric micelles for encapsulation of the anticancer agent 9-nitrocamptothecin HY-16560 (HY-16560). Folic acid-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) is a cyclic heptasaccharide used to deliver hydrophobic agents based on its property of solubilizing non-polar substances. Methyl-β-cyclodextrin is also extensively used as a cholesterol-depleting reagent . Methyl-β-cyclodextrin strongly reduces clathrin-dependent endocytosis . Methyl-β-cyclodextrin blocks cell migrasome formation .
TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of AMPAR. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression .
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 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 .
Biotin-TAT (47-57), a biotin tagged TAT, is a transactivator of transcription. Biotin-TAT (47-57) is one of the most widely used protein transduction domains (PTDs) into different primary cells is ATP- and temperature-dependent, indicating the involvement of endocytosis .
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .
Tat-GluR23Y, scrambled is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .
Tat-GluR23Y, scrambled TFA is the scrambled peptide of Tat-GluR23Y (HY-P2259). Tat-GluR23Y is a synthetic peptide containing tyrosine residues that inhibit AMPAR endocytosis and is effective in the research of long-term depression (LTD) .
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
Prosaptide Tx14(A), a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) increases both ERK1 and ERK2 phosphorylation in Schwann cells .
Prosaptide Tx14(A) TFA, a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells .
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
Tafolecimab (IBI-306) is a human lgG2 monoclonal antibody that specifically binds PCSK-9 and reduces LDL-C levels by inhibiting PCSK-9-mediated endocytosis of the LDL receptor, which in turn enhances clearance of LDL-C and leads to a reduction in LDL-C levels. Tafolecimab may be used in studies of hypercholesterolaemia .
Clemastanin B, a lignin, has potent anti-influenza activities by inhibiting the virus multiplication, prophylaxsis and blocking the virus attachment. Clemastanin B targets viral endocytosis, uncoating or ribonucleoprotein (RNP) export from the nucleus. Clemastanin B has antioxidant and anti-inflammatory activities .
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
NECAP2 protein plays a pivotal role in endocytosis, interacting with adapter protein complexes AP-1 and AP-2, specifically with AP1G1 and AP2A1. Additionally, it connects with GAE domain proteins GGA1, GGA2, and GGA3, participating in a network of interactions that orchestrate endocytic events. NECAP2 emerges as a key regulator in cellular processes associated with membrane trafficking and vesicular transport. NECAP2 Protein, Human (His) is the recombinant human-derived NECAP2 protein, expressed by E. coli , with N-6*His, C-6*His labeled tag. The total length of NECAP2 Protein, Human (His) is 263 a.a., with molecular weight of ~35.0 kDa.
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