cap 2

CAP 2 is an ionizable cationic lipid composed of two cholesterol units linked by a phosphate connector that includes an amino head group.

CAP2 (Cholesterol-amino-phosphate 2) hydrochloride is a lipid within the cholesterol amino phosphate (CAP) family. It is employed in the synthesis of lipid nanoparticles (LNP) for the delivery of mRNA and other efficacious payloads.

mRNACap 2'-O-methyltransferase uses S-adenosylmethionine (SAM) as a methyl donor to add a methyl group at the 2'-O position of the first nucleotide at the 5' end of Cap-0 mRNA, resulting in the formation of a Cap-1 structure. This Cap-1 structure enhances translation efficiency and boosts subsequent protein expression.

Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent nucleic acid endonucleases (CEN) and significantly inhibits influenza A virus RNA polymerase activity.

RU-0415529 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (NSP14), with an IC50 of 356 nM. It inhibits viral RNA methylation and replication by stabilizing the cap-binding pocket through SAH binding. Additionally, RU-0415529 exhibits anti-infective activity in mouse models.

TDI-015051 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (SARS-CoV-2 NSP14) with an IC50 of ≤0.15 nM. It effectively inhibits SARS-CoV-2 NSP14 in Huh-7.5 cells (EC50=11.4 nM) and A549 cells expressing ACE2-TMPRSS2 (EC50=64.7 nM). Additionally, TDI-015051 suppresses other coronaviruses such as α-hCoV-NL63, α-hCoV-229E, and β-hCoV-MERS with IC50 values of 1.7, 2.6, and 3.6 nM, respectively. This compound inhibits viral RNA methylation and replication by binding to a stable SAH-cap pocket and demonstrates anti-infection activity in mouse models.

PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and has antiviral properties with broad-spectrum anti-influenza activity. PAN, as the N-terminal PA subunit of the polymerase-RNA complex, possesses a cap-dependent endonuclease (CEN) active site, facilitating RNA cleavage and initiating the synthesis of new RNA molecules. PAN endonuclease-IN-2 targets both influenza HA and RdRp complexes, thereby disrupting viral entry into host cells and impeding viral replication.

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]

Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor, exhibiting 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, respectively, and possessing anti-oxidant activity[1][2].

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)

7-Methylguanosine 5'-diphosphate (7-Methyl-GDP) sodium, a cap analog, is utilized in the synthesis of mRNA cap analogues[1].

M7G(3'-OMe-5')pppA(2'-OMe) is an analogue used for mRNA cap synthesis in vitro.

eIF4E-IN-6 (Compound 4b), a GMP analog, is designed to inhibit the eIF4E protein's ability to bind to cap mRNA. It demonstrates cytotoxic effects on Caco-2, HepG-2, and MCF-7 cell lines with IC50 values of 31, 27, and 21 μM, respectively [1].

SARS-CoV-2-IN-76 (compound 1) operates as an inhibitor of both nsp14-viral cap N7 methyltransferase and PLpro in severe acute respiratory syndrome coronavirus (SARS-CoV-2) [1].