transfection

DOPE (DOPE) 是一种阳离子脂质体的中性辅助脂质 (helper lipid)，能够与阳离子磷脂结合，增强裸 siRNA 的转染效率。

DOTAP chloride (1,2-Dioleoyl-3-trimethylammonium-propane chloride) 是高效的阳离子脂质，靶点主要是细胞膜上的负电荷成分。DOTAP chloride通过静电作用与带负电荷的核酸 (如DNA、RNA) 结合，形成复合物，从而实现核酸的递送。

DODAP是一种具有低细胞毒性和高转染效率的离子性阳离子脂质，可用于合成脂质体并包裹生物活性分子，如mRNA， siRNA和质粒DNA。

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

Pz-1 是 VEGFR2 和 RET 酪氨酸激酶的抑制剂，可阻断 RET 刺激生长所需的血液供应。

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是一种效能显著的二型RET酪氨酸激酶抑制剂(TKI)。此化合物有效抑制了经过重排的RET激酶以及在带有致癌RET突变等位基因的人类甲状腺癌细胞系中的信号传递。此外，HG-6-63-01能损害含RET致癌突变的磷酸化及其信号传导，同时抑制了经RET C634R和RET M918T突变激活的成纤维细胞和甲状腺癌细胞的增殖，为研究RET致癌激活的癌症提供了新的可能性。

119-23是一种电离性阳离子脂质，主要用于制备体内mRNA传递的脂质纳米粒子(LNPs)。与SM-102或DLin-MC3-DMA的LNPs相比，119-23的LNPs在包裹mRNA报告分子后，显示出在小鼠肌肉中的转染效率更高。此类LNPs在肝脏和脾脏免疫细胞的积累也明显高于含SM-102的LNPs。此外，这种LNPs还能够有效包裹编码人类红细胞生成素(hEPO) mRNA，从而显著提高小鼠血清中hEPO的水平。

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 是转染期间重排激酶 (RET) 的抑制剂，能够用于癌症的研究。

RET-IN-15 是转染期间重排激酶 (RET) 的抑制剂，能够用于癌症的研究。

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 是一种阳离子脂质。DOSPA 制备 DNA 是一种很有前途的转染系统。

14:1 EPC trifluoromethanesulfonate是一种含有单不饱和14:1链的乙基磷脂酰胆碱(EPC)，具有转染活性，可用于活性分子输送。

3'Ome-m7GpppAmpG为具有锁核酸(LNA)分子的三核苷酸帽类似物，显示出显著的翻译效率。作为mRNA疫苗和mRNA转染领域的潜在分子生物学工具，3'Ome-m7GpppAmpG适用于蛋白质生产、基因治疗和抗癌免疫等应用。

3'Ome-m7GpppAmpG ammonium 是一种三核苷酸帽类似物，含锁核酸(LNA)分子，具显著翻译效率。作为潜在的分子生物学工具，3'Ome-m7GpppAmpG ammonium 在mRNA疫苗、mRNA转染领域应用广泛，涵盖蛋白质生产、基因治疗以及抗癌免疫等方面。

AA-T3A-C12 是一种茴香酰胺配体-栓系类脂质 (AA-lipidoid)，能够有效介导大量 RNA 的递送，并促进成纤维细胞的转染和活化。