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.

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

Cefditoren Pivoxil is an orally active antibiotic with broad-spectrum antibacterial properties, and Cefditoren demonstrates potent inhibition against both Gram-negative and Gram-positive bacterial pathogens. Cefditoren exhibits a MIC50 of 0.25–0.5 mg/L against Streptococcus pneumoniae, Cefditoren is widely used for treating respiratory tract infections and skin infections. Cefditoren remains valuable in antimicrobial therapy owing to its favorable pharmacokinetic characteristics and reliable therapeutic efficacy.

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].