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NAB2 is a neuroprotectant that targets the small GTPase Rab1a. NAB2 selectively binds to the GDP-bound form of Rab1a and protects multiple cell types from α-synuclein toxicity by increasing Rab1a expression. Rab1a regulates ER-to-Golgi trafficking and mediates endosomal trafficking events of the E3 ubiquitin ligase Rsp5/Nedd4. NAB2 stimulates ubiquitination of related proteins in a Nedd4-dependent manner and rescues α-synuclein-associated trafficking defects associated with early-onset Parkinson's disease .
YSK 12C4 is an ionizable cationic lipid primarily used to enhance siRNA cellular delivery via multifunctional envelope-type nanodevices (MEND). YSK 12C4 promotes siRNA uptake and endosomal escape, effectively silencing genes in human immune cell lines .
INF7 is a derivative of the N-terminal domain of the HA2 protein and is sensitive to pH. INF7 disrupts the stability of endosomal membranes through a mechanism independent of membrane fusion. INF7 can be used to enhance the endosome escape of complex or liposome-encapsulated proteins. Co-encapsulation of INF7 and molecular imaging probes in liposomes can enhance intracellular signaling and probe retention .
YSK 05 is a pH-sensitive cationic lipid. YSK 05 improves the intracellular trafficking of non-viral vectors. YSK 05-MEND shows significantly good gene silencing activity and hemolytic activity. YSK 05 overcomes the suppression of endosomal escape by PEGylation. YSK 05 effectively enhances siRNA delivery both in vitro and in vivo .
OF-02 is an ionizable lipid for mRNA delivery and a key component of lipid nanoparticles (LNPs). OF-02 is protonated in the acidic endosomal environment to promote endosomal escape of mRNA and efficiently induce protein expression in target cells. OF-02 relies on the pH-responsive membrane fusion properties to form a complex with mRNA and destroy the endosomal membrane structure to achieve mRNA release in the cytoplasm. OF-02 is mainly used in the development of mRNA vaccines, gene editing, and protein replacement therapy[1][2][3].
EGA is an inhibitor that selectively targets the endosomal trafficking pathways. EGA targets the proteins involved in the endosomal trafficking pathways through which multiple toxins and viruses enter cells. EGA exerts its activity by inhibiting the trafficking from early endosomes to late endosomes, blocking the entry of multiple acid-dependent bacterial toxins and viruses into mammalian cells and delaying the lysosomal targeting and degradation of EGFR .
ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research .
ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research .
L16 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. L16 can be used in the preparation of liposomes .
IAJD249 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. IAJD249 can be used in the preparation of liposomes .
IAJD93 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. IAJD93 can be used in the preparation of liposomes .
RM 137-15 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. RM 137-15 can be used in the preparation of liposomes .
Al-28 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. Al-28 can be used in the preparation of liposomes .
1O14 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. 1O14 can be used in the preparation of liposomes .
C16-pHD108 is a pH-responsive nanopore-forming peptide. C16-pHD108 functions as a macromolecule delivery carrier via endosomal membrane nanoporation. C16-pHD108 is promising for research of cancers and neurodegenerative diseases .
306Oi9-cis2 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. 306Oi9-cis2 can be used in the preparation of liposomes .
ML-SA5 is a potent TRPML1 cation channel agonist that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and is more potent than ML-SA1. ML-SA5 has anticancer activity and can inhibit tumour growth .
C16-18:1 PE is a lipid. C16-18:1 PE has the activity of promoting membrane fusion and enhancing endosomal escape, which can significantly improve the delivery efficiency of mRNA. C16-18:1 PE is used in the synthesis of lipid nanoparticles (LNP) .
AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro .
IAJD-97 is a single-component ionizable amphiphilic Janus dendrimer carrier targeting mRNA delivery, which self-assembles into dendrimersomes (DNPs) via pH-responsive mechanisms to efficiently encapsulate and protect mRNA, while facilitating cellular uptake and endosomal escape through ionizable amine groups. IAJD-97 is promising for research of cancers .
ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice .
E10i-494 is an ionizable cationic branched endosomal disruptor (BEND) lipid. E10i-494 can be used to generate lipid nanoparticles (LNPs) for mRNA delivery in vitro. E10i-494 can enhance transfection efficiency .
DSPE-PEG3400-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG2000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG1000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
TAT-HA2 Fusion Peptide is a peptide-based delivery agent that combines the pH-sensitive HA2 fusion peptide from Influenza and the cell-penetrating peptide TAT from HIV. TAT-HA2 Fusion Peptide is a transactivator of transcription and hemaglutanin for endosomal release. TAT-HA2 Fusion Peptide enhances cellular uptake of macromolecules .
DSPE-PEG5000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
(1R,2R)-ML-SI3 is an isomer of ML-SI3 and a potent inhibitor of three isoforms of TRPML. (1R,2R)-ML-SI3 inhibits TRPMLs with IC50s of 1.6 μM (TRPML1), 2.3 μM (TRPML2), and 12.5 μM (TRPML3), respectively .
Mannan is an orally active polysaccharide compound that binds to the mannose receptor (MR). Mannan promotes bacterial uptake and endosomal degradation by binding to MR, thereby enhancing the production of IL-12 in immune cells. Mannan enhances ROS production. Mannan modulates immunity, inhibits Aflatoxin B1 (HY-N6615)-induced toxicity, and reduces lipid .
Galactose-PEG-Cy3 is a Cy3 (HY-D0822) labeled Galactose-PEG conjugate. The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. Cy3 has an emission maximum around 562-570 nm. Galactose-PEG improves drug cellular uptake and reduces endosomal degradation, and can be used in drug delivery .
Glucose-PEG2000-Cy3 is a Cy3 (HY-D0822) labeled Glucose-PEG conjugate. The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. Cy3 has an emission maximum around 562-570 nm. Glucose-PEG improves drug cellular uptake and reduces endosomal degradation, and can be used in drug delivery .
O12-D3-I3 is an ionizable cationic lipid. O12-D3-I3 can be used in the generation of lipid nanoparticles (LNPs) for siRNA delivery in vitro and in vivo. LNPs containing O12-D3-I3 enhances LNP endosomal escape for ferroptosis RNAi therapy of cancer .
Fazirsiran sodium is a second-generation RNAi agent. Fazirsiran sodium consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran sodium can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
Fazirsiran (ARO-AAT) is a second-generation RNAi agent. Fazirsiran consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
L17E is an attenuated cationic amphiphilic lytic (ACAL) peptide that can be used to deliver a variety of macromolecules, including proteins, antibodies, and DNA nanostructures. L17E inserts and cleaves the membrane structure through electrostatic interaction, enabling intracellular escape. The efficiency of L17E-mediated delivery is strongly correlated with the expression level of KCNN4 (the gene encoding the calcium-activated potassium channel KCa3.1). L17E also promotes the cellular uptake of macromolecules by inducing micropinocytosis. L17E can be further optimized and improved through dimerization strategies and in combination with other delivery systems, such as nuclear localization signal peptides and cell membrane-coated nanoparticles .
ALC-0315 (GMP Like) is ALC-0315 (HY-138170) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
DOTAP methylsulfat is a cationic lipid reagent, a cationic derivative of trimethylammonium, linked to two 18-carbon fatty acid tails, each with a single olefin group. DOTAP methylsulfat can self-assemble with negatively charged ions (such as DNA) to form complexes, which can be adsorbed to the cell membrane surface and enter the cell by electrostatic interaction and endocytosis, respectively. DOTAP methylsulfat promotes endosomal membrane fusion with its own hydrophobic domain, releases DNA into the cytoplasm, and exerts gene delivery function. DOTAP methylsulfat can be widely used in research fields such as gene therapy, cell transfection, and non-viral vector design[1][2].
Endosidin-2 (ES2) is a selective inhibitor targeting the conserved exosome subunit EXO70. Endosidin-2 binds to the C-terminal domain of EXO70, inhibiting exocytosis and endosomal recycling, while promoting vacuolar trafficking in plant cells. Endosidin-2 interferes with the EXO70-mediated vesicle-to-plasma membrane anchoring process, leading to abnormal aggregation of auxin transporters (such as PIN2) in the cytoplasm and redirected to vacuolar degradation, while causing abnormal Golgi structure (such as cup-shaped or ring-shaped vesicles cisternae formation). Endosidin-2 can inhibit exocytosis in plant and mammalian cells and is mainly used to study the dynamic regulation of membrane trafficking (such as polar growth, vesicle sorting) .
P9R is an antiviral peptide. P9R has broad-spectrum antiviral activities against the coronaviruses (SARS-CoV-2, MERS-CoV and SARS-CoV), A(H1N1)pdm09, A(H7N9) virus, and rhinovirus. P9R directly binds to viruses and inhibits virus-host endosomal acidification. P9R significantly protects mice from A(H1N1)pdm09 infection without generating drug-resistant virus. P9R can be used for pH-dependent respiratory viruses research .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PE (1,2-POPE; 16:0-18:1 PE) is a phosphatidylethanolamine (PE) lipid. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can induce lipid bilayer to form a hexagonal phase (HII) structure in an acidic environment and promote membrane fusion. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can enhance the endosomal escape ability of lipid nanoparticles (LNPs) and improve the cellular delivery efficiency of nucleic acid drugs such as mRNA. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can be used for LNP carrier targeting of gene therapy and mRNA vaccines .
Glucose-PEG2000-Cy3 is a Cy3 (HY-D0822) labeled Glucose-PEG conjugate. The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. Cy3 has an emission maximum around 562-570 nm. Glucose-PEG improves drug cellular uptake and reduces endosomal degradation, and can be used in drug delivery .
Galactose-PEG-Cy3 is a Cy3 (HY-D0822) labeled Galactose-PEG conjugate. The Cy3 fluorophore is commonly used in applications such as immunolabeling, nucleic acid labeling, fluorescence microscopy, and flow cytometry. Cy3 has an emission maximum around 562-570 nm. Galactose-PEG improves drug cellular uptake and reduces endosomal degradation, and can be used in drug delivery .
ALC-0315 (GMP Like) is ALC-0315 (HY-138170) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
YSK 05 is a pH-sensitive cationic lipid. YSK 05 improves the intracellular trafficking of non-viral vectors. YSK 05-MEND shows significantly good gene silencing activity and hemolytic activity. YSK 05 overcomes the suppression of endosomal escape by PEGylation. YSK 05 effectively enhances siRNA delivery both in vitro and in vivo .
OF-02 is an ionizable lipid for mRNA delivery and a key component of lipid nanoparticles (LNPs). OF-02 is protonated in the acidic endosomal environment to promote endosomal escape of mRNA and efficiently induce protein expression in target cells. OF-02 relies on the pH-responsive membrane fusion properties to form a complex with mRNA and destroy the endosomal membrane structure to achieve mRNA release in the cytoplasm. OF-02 is mainly used in the development of mRNA vaccines, gene editing, and protein replacement therapy[1][2][3].
L16 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. L16 can be used in the preparation of liposomes .
IAJD249 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. IAJD249 can be used in the preparation of liposomes .
IAJD93 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. IAJD93 can be used in the preparation of liposomes .
Al-28 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. Al-28 can be used in the preparation of liposomes .
1O14 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. 1O14 can be used in the preparation of liposomes .
306Oi9-cis2 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. 306Oi9-cis2 can be used in the preparation of liposomes .
ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
RM 137-15 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. RM 137-15 can be used in the preparation of liposomes .
DSPE-PEG3400-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG2000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG1000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG5000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
Mannan is an orally active polysaccharide compound that binds to the mannose receptor (MR). Mannan promotes bacterial uptake and endosomal degradation by binding to MR, thereby enhancing the production of IL-12 in immune cells. Mannan enhances ROS production. Mannan modulates immunity, inhibits Aflatoxin B1 (HY-N6615)-induced toxicity, and reduces lipid .
ALC-0315 (GMP Like) is ALC-0315 (HY-138170) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
DOTAP methylsulfat is a cationic lipid reagent, a cationic derivative of trimethylammonium, linked to two 18-carbon fatty acid tails, each with a single olefin group. DOTAP methylsulfat can self-assemble with negatively charged ions (such as DNA) to form complexes, which can be adsorbed to the cell membrane surface and enter the cell by electrostatic interaction and endocytosis, respectively. DOTAP methylsulfat promotes endosomal membrane fusion with its own hydrophobic domain, releases DNA into the cytoplasm, and exerts gene delivery function. DOTAP methylsulfat can be widely used in research fields such as gene therapy, cell transfection, and non-viral vector design[1][2].
1-Palmitoyl-2-oleoyl-sn-glycero-3-PE (1,2-POPE; 16:0-18:1 PE) is a phosphatidylethanolamine (PE) lipid. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can induce lipid bilayer to form a hexagonal phase (HII) structure in an acidic environment and promote membrane fusion. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can enhance the endosomal escape ability of lipid nanoparticles (LNPs) and improve the cellular delivery efficiency of nucleic acid drugs such as mRNA. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can be used for LNP carrier targeting of gene therapy and mRNA vaccines .
INF7 is a derivative of the N-terminal domain of the HA2 protein and is sensitive to pH. INF7 disrupts the stability of endosomal membranes through a mechanism independent of membrane fusion. INF7 can be used to enhance the endosome escape of complex or liposome-encapsulated proteins. Co-encapsulation of INF7 and molecular imaging probes in liposomes can enhance intracellular signaling and probe retention .
TAT-HA2 Fusion Peptide is a peptide-based delivery agent that combines the pH-sensitive HA2 fusion peptide from Influenza and the cell-penetrating peptide TAT from HIV. TAT-HA2 Fusion Peptide is a transactivator of transcription and hemaglutanin for endosomal release. TAT-HA2 Fusion Peptide enhances cellular uptake of macromolecules .
L17E is an attenuated cationic amphiphilic lytic (ACAL) peptide that can be used to deliver a variety of macromolecules, including proteins, antibodies, and DNA nanostructures. L17E inserts and cleaves the membrane structure through electrostatic interaction, enabling intracellular escape. The efficiency of L17E-mediated delivery is strongly correlated with the expression level of KCNN4 (the gene encoding the calcium-activated potassium channel KCa3.1). L17E also promotes the cellular uptake of macromolecules by inducing micropinocytosis. L17E can be further optimized and improved through dimerization strategies and in combination with other delivery systems, such as nuclear localization signal peptides and cell membrane-coated nanoparticles .
RALA peptide is a cationic amphiphilic delivery agent targeting cell membranes, which forms nanoparticles through electrostatic interactions with anionic drugs. RALA peptide has pH-responsive binding properties, which can enhance the α-helical conformation in an acidic environment and destroy the endosomal membrane, promote the release of drugs into the cytoplasm, and exert efficient intracellular delivery activity. RALA peptide can be used in cancer research (enhancing the activity of bisphosphonates against prostate cancer and breast cancer cells) and bone tissue engineering (promoting osteoblast collagen deposition and extracellular matrix mineralization) .
Pip6a is an arginine-rich cell-penetrating peptide. Pip6a has the ability to deliver associated cargoes across the plasma and endosomal membranes and is stable to serum proteolysis. Pip6a is composed of a hydrophobic core region flanked on each side by arginine-rich domains containing β-alanine and aminohexanoyl spacers. Pip6a-conjugated morpholino phosphorodiamidate oligomer (PMO) dramatically enhanced antisense oligonucleotide (ASO) delivery into striated muscles of myotonic dystrophy (DM1) mice .
C16-pHD108 is a pH-responsive nanopore-forming peptide. C16-pHD108 functions as a macromolecule delivery carrier via endosomal membrane nanoporation. C16-pHD108 is promising for research of cancers and neurodegenerative diseases .
Fazirsiran (ARO-AAT) is a second-generation RNAi agent. Fazirsiran consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
P9R is an antiviral peptide. P9R has broad-spectrum antiviral activities against the coronaviruses (SARS-CoV-2, MERS-CoV and SARS-CoV), A(H1N1)pdm09, A(H7N9) virus, and rhinovirus. P9R directly binds to viruses and inhibits virus-host endosomal acidification. P9R significantly protects mice from A(H1N1)pdm09 infection without generating drug-resistant virus. P9R can be used for pH-dependent respiratory viruses research .
Mannan is an orally active polysaccharide compound that binds to the mannose receptor (MR). Mannan promotes bacterial uptake and endosomal degradation by binding to MR, thereby enhancing the production of IL-12 in immune cells. Mannan enhances ROS production. Mannan modulates immunity, inhibits Aflatoxin B1 (HY-N6615)-induced toxicity, and reduces lipid .
Ragulator Complex Protein LAMTOR3; Late endosomal/Lysosomal Adaptor and MAPK and MTOR Activator 3; MEK-Binding Partner 1; Mp1; Mitogen-Activated Protein Kinase Kinase 1-Interacting Protein 1; Mitogen-Activated Protein Kinase Scaffold Protein 1; LAMTOR3; MAP2K1IP
The MAPKSP1 protein, also known as porphobilinogen deaminase (HMBS), is crucial in the heme biosynthetic pathway and catalyzes the sequential polymerization of four porphobilinogen molecules to form hydroxymethyl bixane. The process begins with the assembly of the dipyrromethane cofactor of porphobilinogen or preuroporphyrinogen. MAPKSP1 Protein, Human (His) is the recombinant human-derived MAPKSP1 protein, expressed by E. coli , with N-6*His labeled tag.
C11orf59; LAMTOR1; Late endosomal/lysosomal adaptor and MAPK and MTOR activator 1; Lipid raft adaptor protein p18; LTOR1_HUMAN; p18; p27Kip1-releasing factor from RhoA; p27RF-Rho; PDRO; PP7157; Protein associated with DRMs and endosomes; Ragulator complex protein LAMTOR1; ragulator complex protein PDRO; Ragulator1; RhoA activator C11orf59
The LAMTOR1 protein is an important component of the Ragulator complex and plays dual roles in amino acid sensing and mTORC1 activation. It acts as a guanine nucleotide exchange factor (GEF) for Rag GTPases and mediates their recruitment to the lysosomal membrane. LAMTOR1 Protein, Human (His) is the recombinant human-derived LAMTOR1 protein, expressed by E. coli , with N-His labeled tag.
YSK 05 is a pH-sensitive cationic lipid. YSK 05 improves the intracellular trafficking of non-viral vectors. YSK 05-MEND shows significantly good gene silencing activity and hemolytic activity. YSK 05 overcomes the suppression of endosomal escape by PEGylation. YSK 05 effectively enhances siRNA delivery both in vitro and in vivo .
OF-02 is an ionizable lipid for mRNA delivery and a key component of lipid nanoparticles (LNPs). OF-02 is protonated in the acidic endosomal environment to promote endosomal escape of mRNA and efficiently induce protein expression in target cells. OF-02 relies on the pH-responsive membrane fusion properties to form a complex with mRNA and destroy the endosomal membrane structure to achieve mRNA release in the cytoplasm. OF-02 is mainly used in the development of mRNA vaccines, gene editing, and protein replacement therapy[1][2][3].
Al-28 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. Al-28 can be used in the preparation of liposomes .
1O14 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. 1O14 can be used in the preparation of liposomes .
306Oi9-cis2 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. 306Oi9-cis2 can be used in the preparation of liposomes .
ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine .
RM 137-15 is an ionizable lipid. The ability of ionizable lipids to form unstable non-bilayer structures at acidic pH is key for endosomal escape and cytosolic delivery of RNA. RM 137-15 can be used in the preparation of liposomes .
DSPE-PEG2000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG1000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
DSPE-PEG5000-MPG is a PEG compound which composed of DSPE and a peptide vector (MPG). MPG is derived from both the nuclear localisation sequence (NLS) of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41. MPG could deliver short oligonucleotides into cells efficiently and independently of the endosomal pathway .
Fazirsiran sodium is a second-generation RNAi agent. Fazirsiran sodium consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran sodium can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
Fazirsiran (ARO-AAT) is a second-generation RNAi agent. Fazirsiran consistes of a cholesterol-conjugated RNAi trigger (chol-RNAi) to selectively degrade Alpha1-antitrypsin (AAT) mRNA by RNAi and a melittin-derived peptide conjugated to N-acetylgalactosamine (NAG) formulated as the excipient EX1 to promote endosomal escape of the chol-RNAi in hepatocytes . Fazirsiran can be used in the study of Alpha-1 Antitrypsin Deficiency (AATD) liver disease.
DOTAP methylsulfat is a cationic lipid reagent, a cationic derivative of trimethylammonium, linked to two 18-carbon fatty acid tails, each with a single olefin group. DOTAP methylsulfat can self-assemble with negatively charged ions (such as DNA) to form complexes, which can be adsorbed to the cell membrane surface and enter the cell by electrostatic interaction and endocytosis, respectively. DOTAP methylsulfat promotes endosomal membrane fusion with its own hydrophobic domain, releases DNA into the cytoplasm, and exerts gene delivery function. DOTAP methylsulfat can be widely used in research fields such as gene therapy, cell transfection, and non-viral vector design[1][2].
1-Palmitoyl-2-oleoyl-sn-glycero-3-PE (1,2-POPE; 16:0-18:1 PE) is a phosphatidylethanolamine (PE) lipid. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can induce lipid bilayer to form a hexagonal phase (HII) structure in an acidic environment and promote membrane fusion. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can enhance the endosomal escape ability of lipid nanoparticles (LNPs) and improve the cellular delivery efficiency of nucleic acid drugs such as mRNA. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PE can be used for LNP carrier targeting of gene therapy and mRNA vaccines .
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