spike

The COVID-19 Spike Protein mRNA, responsible for expressing the COVID-19 spike protein, is crucial for evaluating RNA delivery, translation efficiency, and cell viability. Positioned on the membrane surface, this spike protein facilitates virus entry into cells by binding to host cell membrane receptors and promoting membrane fusion. It serves as a significant action site for neutralizing antibodies and represents a primary focus in vaccine development [1].

Anti-SARS-CoV-2 Spike mAb (CR3022) is a human monoclonal IgG1 antibody produced from CHO cells, which specifically targets the S1 domain of the Spike protein in both SARS-CoV and SARS-CoV-2.

COVID-19 Spike Protein mRNA-LNP is a lipid nanoparticle (LNP) formulated with the novel coronavirus pneumonia spike protein, positioned on the membrane surface. It is designed for applications such as RNA delivery, translation efficiency, and cell viability assessment. This spike protein facilitates the COVID-19 virus's entry into host cells by binding to cell membrane receptors and enabling membrane fusion, making it a critical focal point for host neutralizing antibodies and vaccine development [1].

Anti-Spike-RBD mAb is a CHO cell-derived human monoclonal IgG1 antibody that potentially treats SARS-CoV-2 by blocking the interaction between the spike protein and ACE2[1].

The Anti-Spike-RBD Single Domain mAb is a monoclonal antibody derived from CHO cells in Alpaca. It is composed of VHH-huFc and exhibits a strong affinity for the SARS-CoV-2 RBD. [1]

Spike Binding Peptide 1 (SBP1), representing amino acids 21-43 of angiotensin-converting enzyme 2 (ACE2), has been utilized in a novel approach involving lipid nanoparticles (LNPs) encapsulated with oseltamivir phosphate and conjugated to SBP1. This formulation aims to investigate the possibility of achieving a controlled, long-term in vivo release of oseltamivir phosphate. Furthermore, a 2% concentration of SBP1 immobilized on crosslinked networks composed of hydroxy acrylate and ethylxanthate ethyl acrylate has demonstrated enhanced in vitro efficiency in capturing the spike glycoprotein of severe acute respiratory coronavirus 2 (SARS-CoV-2), also referred to as the surface glycoprotein.

Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis.

Emodin (Frangula emodin) is a naturally occurring anthraquinone present in the roots and barks of numerous plants; exerts antiproliferative effects in Y cells that are regulated by different signaling pathways.

PLpro/RBD-IN-1 is a dual inhibitor of SARS-CoV-2 PLpro and the spiny protein RBD, with anti-novel coronavirus activity, and is seen for the study of viral infections.

Dendrotoxin K, a Kv1.1 channel blocker, modulates glutamate release in CA3 neurons by regulating the presynaptic spike waveform in a time-dependent manner [1].

SSAA09E2 is a new SARS-CoV replication inhibitor, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2).

CAY10781 is an inhibitor of the protein-protein interaction between neuropilin-1 (NRP-1) and VEGF-A.1It inhibits the interaction by 43% when used at a concentration of 12.5 μM. CAY10781 also inhibits VEGF-A-induced phosphorylation of VEGFR2 in catecholamine A-differentiated (CAD) cells when used at the same concentration. 1.Perez-Miller, S., Patek, M., Moutal, A., et al.In silico identification and validation of inhibitors of the interaction between neuropilin receptor 1 and SARS-CoV-2 Spike proteinbioRxiv308783(2020)

Human ACE2 receptor-derived 23-amino acid peptide. Binds receptor binding domain (RBD) of insect-derived SARS-CoV-2 spike protein (KD = 1.3 μM for N-terminal biotinylated, insect-derived spike protein RBD; see Zhang et al preprint publication). Please note - unpublished, in-house data suggests approximately 75-fold lower affinity for insect-derived SARS-CoV-2 RBD than reported by Zhang et al.

Anti-SARS-80R mAb (SARS-80R) is a human IgG1 monoclonal antibody derived from CHO cells, designed to selectively bind the Spike (S1) protein, thereby preventing SARS virus infection in susceptible cells[1].

SARS-CoV-2-IN-29 disodium, a diphosphate ester featuring a benzene system and molecular tweezers architecture, demonstrates antiviral efficacy by targeting SARS-CoV-2 with half-maximal inhibitory concentrations (IC50s) of 1.5 μM for virus activity and 1.6 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, evidenced by a half-maximal effective concentration (EC50) of 3.0 μM [1].

SARS-CoV-2-IN-30 disodium, a benzene-system-based two-armed diphosphate ester featuring molecular tweezers, demonstrates antiviral efficacy, with IC50 values of 0.6 μM against SARS-CoV-2 and 6.9 μM for spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes, evidenced by an EC50 of 6.9 μM [1].

SARS-CoV-2-IN-28 disodium, a diphosphate ester featuring a C7 alkyl chain and extended-length molecular tweezers, demonstrates antiviral efficacy by showing IC50 values of 0.4 μM and 1.0 μM against SARS-CoV-2 activity and spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes with an EC50 of 4.4 μM [1].

SARS-CoV-2-IN-30, a two-armed diphosphate ester featuring a benzene system and molecular tweezers, demonstrates antiviral properties, achieving IC50 values of 0.6 μM against SARS-CoV-2 activity and 6.9 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes with an EC50 of 6.9 μM [1].

SARS-CoV-2-IN-23 disodium, a medium-length molecular tweezer and two-armed diphosphate ester, demonstrates antiviral properties by inhibiting SARS-CoV-2 activity and spike pseudoparticle transduction with IC50 values of 8.2 μM and 2.6 μM, respectively. Additionally, it disrupts liposomal membranes with an EC50 of 4.4 μM [1].

SARS-CoV-2-IN-25 (Compound CP026) disodium, a potent inhibitor of SARS-CoV-2 spike pseudoparticle transduction, demonstrates significant efficacy with an IC50 value of 1.6 μM. It also effectively inhibits enveloped viruses and liposomes, highlighting its broad-spectrum antiviral potential.

SARS-CoV-2-IN-64 (compound 9), derived from chenodeoxycholic acid, is a potent inhibitor of the SARS-CoV-2 spike glycoprotein [1].

Masavibart (ZRC3308-A7), an IgG1 type anti-SARS-CoV-2 monoclonal antibody, demonstrates strong binding affinity for a distinct non-competing epitope located on the receptor-binding domain (RBD) of the SARS-CoV-2 spike protein. When paired in a 1:1 ratio with ZRC3308-B10, Masavibart is efficacious in preventing COVID-19, particularly in its early stages before the onset of severe symptoms [1].

Ogalvibart (C-135-LS), a humanized anti-SARS-CoV-2 IgG1 type monoclonal antibody, specifically targets and binds to the spike (S) glycoprotein receptor-binding domain (RBD) of the SARS-CoV-2 virus. When combined with C144LS in a 1:1 ratio, Ogalvibart demonstrates significant preventive activity and effectively prevents the progression of COVID-19 in a rhesus monkey disease model [1].

Regdanvimab (CT-P59) is a human monoclonal antibody targeting the receptor-binding domain of the SARS-CoV-2 spike protein, inhibiting the virus's cell entry by blocking its interaction with the ACE2 receptor. It is utilized in COVID-19 research [1].

Romlusevimab (BRII-198) is a human IgG1 monoclonal antibody that neutralizes the SARS-CoV-2 spike protein, targeting the virus responsible for severe acute respiratory syndrome [1] [2].

Lomtegovimab (BI 767551), a humanized monoclonal antibody targeting the SARS-CoV-2 spike glycoprotein, exhibits antiviral efficacy by binding to and neutralizing the virus. This compound holds potential for COVID-19 research [1] [2].

SARS-CoV-2-IN-27 disodium, a diphosphate ester featuring a C6 alkyl chain and molecular tweezers of extended length, demonstrates antiviral efficacy by achieving IC50 values of 1.0 μM against SARS-CoV-2 activity and 1.7 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, displaying an EC50 value of 6.5 μM [1].

SARS-CoV-2-IN-23, a two-armed diphosphate ester and medium-length molecular tweezers, displays antiviral properties, demonstrating IC50 values of 8.2 μM against SARS-CoV-2 activity and 2.6 μM for spike pseudoparticle transduction. Additionally, it induces liposomal membrane disruption with an EC50 value of 4.4 μM [1].

Dendrotoxin K TFA, a Kv1.1 channel blocker, modulates glutamate release in CA3 neurons by time-dependently regulating the presynaptic spike waveform [1].

Simaravibart (MAD-0004J08), an IgG1κ monoclonal antibody, specifically targets the receptor-binding domain of the SARS-CoV-2 spike (S) glycoprotein [1].

Beludavimab (BMS 4182137; VIR 7832), a monoclonal antibody, specifically targets the spike glycoprotein of SARS-CoV-2, effectively binding to the receptor-binding domain of the recombinant spike protein (S-RBD) with an equilibrium concentration (EC50) of 14.9 ng mL and a dissociation constant (Kd) of 0.21 nM [1].

CPD7 HCl is a novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein.

SARS-CoV-2-IN-27, a diphosphate ester featuring a C6 alkyl chain and extended-length molecular tweezers, demonstrates antiviral efficacy, with IC50 values of 1.0 μM and 1.7 μM against SARS-CoV-2 activity and spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes, evidenced by an EC50 of 6.5 μM [1].

SARS-CoV-2-IN-29, a two-armed diphosphate ester featuring a benzene system and molecular tweezers, demonstrates antiviral efficacy with IC50 values of 1.5 μM for SARS-CoV-2 activity and 1.6 μM against spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, as indicated by an EC50 of 3.0 μM [1].

SARS-CoV-2-IN-34 (S-20-1) is a broad-spectrum pan-coronavirus (CoV) fusion inhibitor that penetrates the blood-brain barrier and exhibits extensive inhibitory activity against both pseudotyped and authentic SARS-CoV-2, as well as pseudotyped variants of concern (VOCs). It shows high affinity for the receptor-binding domain (RBD) in the S1 and the heptad repeat 1 (HR1) domain in the S2 of the SARS-CoV-2 spike (S) protein, making it a valuable tool for infection research [1].

DMJ-I-228 is a specific inhibitor of HIV-1 entry through interaction with the Env spike by virtue of the incorporation of a guandinium group.

Anti-MERS-3A1 mAb (MERS-3A1) is a high-affinity human IgG1 monoclonal antibody derived from CHO cells that effectively inhibits the interaction between the MERS-CoV spike protein and the DPP4 receptor[1].

SIMR3030, a potent inhibitor of SARS-CoV-2 PLpro, possesses an IC50 of 0.0399 µg mL and demonstrates antiviral activity by diminishing the expression of SARS-CoV spike, ORF1b, IFN-α, and IL-6 mRNA. Additionally, SIMR3030 has been shown to have a satisfactory safety profile in mice [1].

C12-113, a lipidoid delivery agent, effectively transfects siRNA into cells and, when combined with additional lipids, forms lipid nanoparticles (LNPs). These LNPs facilitate the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice [1] [2].

CPD26 is a novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein.

SARS-CoV-2-IN-25 (Compound CP026) is a potent inhibitor of SARS-CoV-2 spike pseudoparticle transduction, with an inhibitory concentration (IC50) of 1.6 μM. It effectively inhibits both enveloped viruses and liposomes [1].

Anti-MERS-2E6 mAb (MERS-2E6), a human IgG1 neutralizing antibody expressed in CHO cells, effectively competes with the virus Spike protein for binding to the CD26 receptor, thereby inhibiting viral invasion into host cells.

SARS-CoV-2-IN-51 (S-10), a lead compound for Omicron fusion inhibition, demonstrates potent activity against Omicron and other SARS-CoV-2 variants, with EC50 values ranging from 0.82-5.45 μM. It functions by directly interacting with the spike (S) protein in the prefusion state [1], thereby preventing viral entry.

Crexavibart (BMS-986413; C-144-LS), an IgG1 λ2 antibody, specifically targets the receptor-binding domain of the SARS-CoV-2 spike (S) glycoprotein [1].

Nepuvibart (ZRC3308-B10), an IgG1 type anti-SARS-CoV-2 monoclonal antibody, exhibits strong binding affinity to a distinct non-competing epitope on the receptor-binding domain (RBD) of the SARS-CoV-2 spike protein. When combined in a 1:1 ratio with ZRC3308-A7, Nepuvibart is effective in preventing COVID-19 and in treating the early stages of the disease before it progresses to severe illness [1].

Anti-MERS-D12 mAb (MERS-D12; MERS Antibody-D12) is a human monoclonal IgG1 that specifically targets the DPP4 interacting region of the MERS-CoV Spike receptor binding domain (RBD), effectively neutralizing the virus by blocking its ability to bind to receptors [1].

AA 497, a beta-2 agonist, causes relaxation and suppresses Ca spike frequency.

CPD7 is a novel non-RBD binding modulator to inhibit SARS-CoV-2 by prohibiting the conformational change of the spike (S) protein.

Fluorescently labelled peptide derived from human ACE2 (SBP1, Cat. No. 7233). Composed of SBP1 conjugated to FITC (Fluorescein-5-isothiocyanate; Cat. No. 5440). SBP1 binds receptor binding domain (RBD) of insect-derived SARS-CoV-2 spike protein (KD = 1.3 μM for N-terminal biotinylated, insect-derived spike protein RBD; see Zhang et al preprint publication). Please note - unpublished, in-house data suggests SBP1 has approximately 75-fold lower affinity for insect-derived SARS-CoV-2 RBD than reported by Zhang et al.

SARS-CoV-2-IN-28, a two-armed diphosphate ester featuring a C7 alkyl chain and molecular tweezers of extended length, demonstrates antiviral properties by exhibiting IC 50 values of 0.4 μM against SARS-CoV-2 activity and 1.0 μM against spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, evidenced by an EC 50 value of 4.4 μM [1].