transfection

DOPE (DOPE) is a neutral helper lipid for cationic liposomes.It is used in combination with cationic phospholipids to increase efficiency during DNA transfection studies as a non-viral method of gene delivery.

DOTAP chloride (1, 2-dioleoyl-3-trimethylammonium-propane chloride) is an efficient cationic lipid, and its target is mainly the negatively charged components on the cell membrane. DOTAP chloride binds to negatively charged nucleic acids (such as DNA and RNA) by electrostatic interaction to form complexes, thereby achieving the delivery of nucleic acids.

DODAP is an ionic cationic lipid with low cytotoxicity and high transfection efficiency that can be used to synthesize liposomes and encapsulate biologically active molecules such as mRNA, siRNA and plasmid DNA.

trans-Pralsetinib (trans-BLU-667) is an inhibitor of rearranged during transfection (RET).

Pz-1 is an inhibitor of VEGFR2 and RET (rearranged during transfection) tyrosine kinase that blocks the blood supply required for RET-stimulated growth.

Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a

HG-6-63-01 serves as a type II RET tyrosine kinase inhibitor (TKI). It effectively targets and inhibits REarranged during Transfection (RET) kinase, disrupting signaling pathways in human thyroid cancer cell lines possessing oncogenic RET alleles. Moreover, this compound reduces the phosphorylation and signaling of RET oncogenic mutants. HG-6-63-01 further suppresses the proliferation of fibroblasts transformed by RET/C634R and RET/M918T, as well as thyroid cancer cells with RET mutations, showing potential as a therapeutic option for cancers with oncogenic activation of RET.

119-23 is an ionizable cationic lipid frequently utilized in the preparation of lipid nanoparticles (LNPs) for in vivo mRNA delivery. Lipid nanoparticles that include 119-23 and encapsulate mRNA reporter molecules demonstrate a higher transfection efficiency in mouse muscle compared to LNPs containing SM-102 or DLin-MC3-DMA. Additionally, the accumulation of 119-23-containing LNPs in immune cells within the liver and spleen of mice is significantly greater than that of LNPs with SM-102. Furthermore, LNPs containing 119-23 and encoding human erythropoietin (hEPO) mRNA can elevate serum hEPO levels in mice.

FHND5071 (1H) is a selective inhibitor of RET (rearranged during transfection) tyrosine kinase. It shows potential for research applications in RET-driven cancers, such as thyroid and lung cancer.

ISD (interferon stimulatory DNA) sodium is a 45 bp double-stranded non-CpG oligomer derived from the genome of Listeria monocytogenes. Upon transfection into cells, ISD sodium significantly boosts the expression of IFN-β. This ISD-induced response is mediated by the STING-TBK1-IRF3 signaling pathway.

Lipofectin is used to promote the transfection of plasmid vectors in vitro and in vivo.

H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection efficiency.4 1.Park, H.S., Kim, C., and Kang, Y.K.Preferred conformations of RGDX tetrapeptides to inhibit the binding of fibrinogen to plateletsBiopolymers63(5)298-313(2002) 2.Tranqui, L., Andrieux, A., Hudry-Clergeon, G., et al.Differential structural requirements for fibrinogen binding to platelets and to endothelial cellsJ. Cell Biol.108(6)2519-2527(1989) 3.Ferris, D.M., Moodie, G.D., Dimond, P.M., et al.RGD-coated titanium implants stimulate increased bone formation in vivoBiomaterials20(23-24)2323-2331(1999) 4.Kunath, K., Merdan, T., Hegener, O., et al.Integrin targeting using RGD-PEI conjugates for in vitro gene transferJ. Gene Med.5(7)588-599(2003)

Cho-Arg is a steroid-based cationic lipid that contains a cholesterol skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratios greater than or equal to 4. Cho-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence or absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It is cytotoxic to H1299 cells (IC50 = 88.5 μg/ml).

Dios-Arg is a steroid-based cationic lipid that contains a diosgenin skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratio greater than or equal to 4. Dios-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence and absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It has been used, coupled to 1,2-dioleoyl-sn-glycero-3-PE , to bind siRNA and plasmid DNA to form cationic lipid nanoparticles for intracellular transport. Dios-Arg is cytotoxic to H1299 and HeLa cells (IC50s = 83.5 and 74.1 μg/ml, respectively).

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).

PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neuronal input transformations by tunable dendritic inhibition. Nat.Neurosci. 15 423 PMID:22246433 |Satoh et al (2016) Context-dependent gait choice elicited by EphA4 mutation in Lbx1 spinal interneurons. Neuron 89 1046 PMID:26924434 |Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Nature 488 172 PMID:22801496 |Hirschberg et al (2017) Functional dichotomy in spinal- vs prefrontal-projecting locus coeruleus modules splits descending noradrenergic analgesia from ascending aversion and anxiety in rats. Elife 6 e29808 PMID:29027903

DMPAC-Chol is a cationic cholesterol derivative that has been used in liposome formation for gene transfection. Liposomes containing DMPAC-chol bind to DNA in a band shift assay and protect against serum nuclease degradation of DNA when used at lipsome:DNA ratios ranging from 2.5:1 to 10:1 w/w. DMPAC-Chol-containing liposomes also reduce viability of HepG2 cells by 63% when used at a concentration of 37.5 μg/ml.

KALA, an amphiphilic peptide, adopts an α-helical conformation under physiological pH conditions. It functions as a fusogenic peptide, modifying the liposomal membrane that encapsulates plasmid DNA, thereby facilitating liver targeting and DNA transfection through galactose receptors.

RET-IN-8 is an inhibitor of rearrangement kinase (RET) during transfection and can be used in cancer research.

RET-IN-15 is an inhibitor of rearrangement kinase (RET) during transfection and can be used in cancer research.

SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.

DOSPA, a cationic lipid, exhibits significant potential when formulated with DNA as a transfection system [1].

14:1 EPC trifluoromethanesulfonate, an ethyl-phosphatidylcholine (EPC) derivative with monounsaturated 14:1 chains, exhibits transfection activity. This compound is utilized for drug delivery [1] [2].

3'Ome-m7GpppAmpG, a trinucleotide cap analogue with a locked nucleic acid (LNA) molecule, demonstrates notable translational efficiency. It serves as a promising tool in molecular biology, applicable in mRNA vaccines and transfection processes, including protein production, gene therapy, and anti-cancer immunization [1].