cap 2

CAP 2是一个可电离阳离子脂质，由两个胆固醇部分通过含有氨基头基的磷酸连接器连接而成。

CAP2 (Cholesterol-amino-phosphate 2) hydrochloride 是一种胆固醇氨基磷酸盐 (CAP) 类脂质，主要用于制备脂质纳米颗粒 (LNP)，这些颗粒可用于传递mRNA及其他生物有效载荷。

Cap-dependent endonuclease-IN-2 是一种 cap-dependent 核酸内切酶 (CEN) 的有效抑制剂。Cap-dependent endonuclease-IN-2 对流感病毒具有很好的抑制作用，且细胞毒性较低，具有较好的体内药剂动力学特性和体内药效学特性。Cap-dependent endonuclease-IN-2 能够明显的抑制甲型流感病毒 RNA 聚合酶活性。

XR 1853 is a low molecular weight modulator of human plasminogen activator inhibitor-1 activity.

7-Methylguanosine 5’-diphosphate (7-Methyl-GDP) sodium, a cap analog, can be used in the synthesis of mRNA cap analogues[1]. 7-Methylguanosine 5’-diphosphate sodium inhibits binding of eukaryotic initiation factors to reovirus capped mRNA and complex formation involving uncapped mRNA or 18 S rRNA[1].T. brucei mRNA decapping enzyme (TbDcp2) that cleaves 7-Methylguanosine 5’-diphosphate sodium from capped RNA to generate pRNA, a substrate for TbCe1[2]. [1]. Sonenberg N, et al. Nonspecific effect of m7GMP on protein-RNA interactions. J Biol Chem. 1978;253(19):6630-6632.[2]. Ignatochkina AV, et al. The messenger RNA decapping and recapping pathway in Trypanosoma. Proc Natl Acad Sci U S A. 2015;112(22):6967-6972.

Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A Puerto Rico 8 34 (H1N1) and A Aichi 2 68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2]. Methyl brevifolincarboxylate exhibits significant DPPH radical scavenging activity with an IC50 value of 8.9 μM. [1]. Wu QY, et al. Chromatographic fingerprint and the simultaneous determination of five bioactive components of geranium carolinianum L. water extract by high performance liquid chromatography. Int J Mol Sci. 2011;12(12):8740-8749. [2]. Fang SH, et al. Anti-oxidant and inflammatory mediator's growth inhibitory effects of compounds isolated from Phyllanthus urinaria. J Ethnopharmacol. 2008;116(2):333-340.

Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino cap group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm

1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) is a biotinylated phospholipid. It has been used in PEGylated polyamidoamine-dendrimer-conjugated supported lipid bilayers (SLB) to isolate circulating tumor cells and tumor cell microembolis from patient-derived blood by antibody-coated microfluidics. [1] It has also been used as a component of SLBs to detect protein-ligand binding with ortho-conjugated Texas Red DHPE. [2] In addition, 1,2-dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) has been used in SLBs partitioned into nanowells to create DNA curtains, which can be used as a high-throughput tool for detection of protein-DNA interactions at the single molecule level.[3]

2',3'-O-Isopropylideneguanosine is an alkylated guanosine building block.1,2It has been used in the synthesis of ordered honeycomb microporous films and mRNA cap analogs. 1.Gao, Y.-F., Huang, Y.-J., Xu, S.-Y., et al.Ordered honeycomb microporous films from self-assembly of alkylated guanosine derivativesLangmuir27(6)2958-2964(2011) 2.Kore, A.R., Shanmugasundaram, M., and Vlassov, A.V.Synthesis and application of a new 2',3'-isopropylidene guanosine substituted cap analogBioorg. Med. Chem. Lett.18(17)4828-4832(2008)

RU-0415529 是一种可口服的 SARS-CoV-2 非结构蛋白 14 (NSP14) 抑制剂，IC50为 356 nM。该化合物通过结合 SAH 稳定的 cap 结合口袋，抑制病毒 RNA 甲基化和病毒复制。在小鼠模型中，RU-0415529 展示了显著的抗感染活性。

SARS-CoV-2-IN-76 (compound 1) 作为一种nsp14 病毒帽 N7 甲基转移酶及PLpro抑制剂，主要应用于研究严重急性呼吸综合征冠状病毒 (SARS-CoV-2)。

eIF4E-IN-6（化合物4b）是一种针对eIF4E设计的抑制剂，可阻止其与cap mRNA的结合，其化学结构为GMP类似物。该化合物在Caco-2、HepG-2和MCF-7细胞系中显示出细胞毒性效果，其IC50值分别约为31、27和21 μM。

M7G(3'-OMe-5')pppA(2'-OMe) 是一种帽子类似物，用于 mRNA 的体外合成。

TDI-015051 是一种口服有效的 SARS-CoV-2 非结构蛋白 14 (SARS-CoV-2 NSP14) 抑制剂，IC50≤0.15 nM。在 Huh-7.5 细胞 (EC50=11.4 nM) 和表达 ACE2-TMPRSS2 的 A549 细胞 (EC50=64.7 nM) 中能够抑制 SARS-CoV-2 NSP14。此外，TDI-015051 对其他冠状病毒，如 α-hCoV-NL63、α-hCoV-229E 和 β-hCoV-MERS，也有抑制作用，IC50分别为 1.7、2.6 和 3.6 nM。通过与SAH稳定的cap口袋结合，TDI-015051 可抑制病毒 RNA 甲基化和病毒复制，并在小鼠模型中显示出抗感染活性。