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，可以在不使用辅助脂质的情况下，作用于瞬时或者稳定转染 DNA (质粒、bacmids) 和修饰核酸 (反义寡核苷酸)。

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。

RCB-02-4-8，一种可电离的阳离子脂质，主要用于构建脂质纳米颗粒(LNPs)以传递mRNA，能有效提升小鼠肺部的转染效率。

DC-6-14为一种阳离子脂类，用于合成脂质体，具备基因转染活性。

HBpep(RPY)-SP 是 HBpep-SP 的多肽变体，与脂质双分子层相互作用。该化合物在原代细胞和免疫细胞等难以转染的细胞中表现出卓越的转染效率。HBpep(RPY)-SP 适用于蛋白质、基因和免疫细胞疗法的研究。

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。

DORI为一种阳离子脂质，能够在体外传递质粒DNA，具有低细胞毒性和高转染效率特性。

The a-helix of the amphipathic peptide antibiotic LAH4 (KKALLALALHHLAHLALHLALALKKA-NH2) strongly interacts with phospholipid membranes, demonstrating in vitro transfection efficiencies comparable to those of commercially available reagents.

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

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).

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。

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。

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。

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。

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。

ppTG20，一种两亲性细胞穿透肽 (KALA)，主要应用于基因转染。该肽与 DNA 结合后，能够破坏细胞膜的稳定性，从而促进 DNA 的成功转染。

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。

3-Azidopropylamine，一种含叠氮基团的点击化学试剂，能够与马铃薯淀粉中的淀粉糖发生反应，用于质粒DNA的络合及转染。

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).

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)

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.

GL67 (N4-Spermine cholesteryl carbamate)为一种阳离子脂质，用于核酸活性分子、疫苗的递送及基因转染。

DOTMA (N-(1-(2,3-dioleyloxy)propyl)-N,N,N-trimethylammonium) 作为 tetra-methylated DOTA 类似物，是一种阳离子脂类，被用作基因治疗的非病毒载体。它已被用作脂质体的成分，可用于封装 siRNA、microRNA 和寡核苷酸，并用于体外基因转染。在体外和体内均表现出良好的基因转染效果。DOTMA 诱导脂质体上的正电荷，从而促进脂质体与细胞膜的有效相互作用。