SARS CoV IN 3

SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication.

SARS-CoV-2 nsp13-IN-3 (Compound C3) is a small molecule inhibitor of SARS-CoV-2 non-structural protein 13 (nsp13), targeting nsp13 ssDNA+ATPase with an IC50 of 32 μM.

SARS-CoV-2 3CLpro-IN-3, a SARS-CoV-2 3CLpro inhibitor, demonstrates antiviral, antibacterial, and antifungal properties.

SARS-CoV-2 nsp14-IN-3 (4975) is a potent inhibitor of the N7-Methyltransferase activity of SARS-CoV-2 nonstructural protein 14 (Nsp14), with an IC50 value of 3.5 μM [1].

Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against enveloped and non-enveloped viruses, suppressing virus propagation and modulating the expression of inflammatory cytokines for use as an anti-influenza virus agent [3]. It effectively inhibits the fusion of the virus with host cells [1] [2] and is an efficient inhibitor of SARS-CoV-2 in vitro [2].

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity that inhibits the replication of severe acute respiratory syndrome coronavirus [SARS-CoV] in Vero 76 cells, Middle East respiratory syndrome coronavirus [MERS-CoV] in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s = 0.1, 0.15, and 0.3 μM, respectively).

SARS-CoV-2-IN-14 is a potent and oral inhibitor of SARS-CoV-2 (IC50:0.39 μM), which is an analogue of niclosamide. SARS-CoV-2-IN-14 was more stable than niclosamide in the determination of human plasma and liver S9 enzyme. Oral administration of SARS-CoV-2-IN-14 can improve its bioavailability and half-life.

CathepsinL-IN-5 (D6-3) is a potent inhibitor of Cathepsin L (CatL) with an IC50 value of 0.27 nM. It effectively blocks the function of CatL and significantly impedes the entry of SARS-CoV-2 pseudovirus into cells by inhibiting the cleavage of the spike protein. CathepsinL-IN-5 is applicable for research on infections.

3CLPro-IN-3 (Compound A36) is an inhibitor of SARS-CoV-2 3CLpro with an IC50 value of 51.3 nM. It exhibits antiviral activity against human coronaviruses 229E, OC43, and the murine coronavirus MHV.

9-AMN is an inhibitor of the SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro), effectively reducing its deubiquitinating (DUB) activity and protease activity, with IC50 values of 4.55 µM and 4.15 µM, respectively. Additionally, 9-AMN suppresses the replication of the SARS-CoV variants Delta and Omicron in Calu-3 cells, with IC50 values of 1.04 µM and 2.35 µM, respectively.

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

CCF0058981 (CCF981) is a 3-chlorophenyl analogue, serving as a noncovalent inhibitor of SARS-CoV-2 3CL pro (SC2), demonstrating potent activity with an IC50 of 68 nM. It also exhibits inhibitory effects against SARS-CoV-1 3CL pro (SC1) with an IC50 of 19 nM, highlighting its antiviral efficacy and potential in COVID-19 research [1].

SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective, and irreversible inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 value of 116 nM [1].

3CPLro-IN-1 (compound A17) is a potent, orally active inhibitor of SARS-CoV-2 3-Chymotrypsin-like cysteine protease (3CLpro) with an IC50 of 5.65 μM, making it an attractive drug target against COVID-19 and also considered an antitumor agent-51.

SARS-CoV-2 nsp14-IN-1 (Compound 3) is a dual-substrate inhibitor of SARS-CoV-2 Nsp14 Mtase with an IC50 of 0.061 μM, targeting substrates such as histone lysine, protein arginine, DNA, and RNA.

SARS-CoV-2-IN-33 is an inhibitor of COVID-19. SARS-CoV-2-IN-3 exhibits good binding affinity (-8.0 Kcal mole) for COVID-19 major protease (Mpro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 exhibits good anti-proliferative effects on cancer cells. SSARS-CoV-2-IN-33 can be used to study cancer and COVID-19.

3CPLro-IN-2 is a potent, orally active inhibitor of SARS-CoV-2 3CLpro (IC50: 1.55 μM, Ki: 6.09 μM). 3-Chymotrypsin-like cysteine protease (3CLpro) is an essential protein for viral replication and is a potential drug target against COVID-19.

Camostat, also known as FOY 305, is a serine protease inhibitor. Camostat is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. In vitro study showed that camostat significantly reduces the infection of Calu-3 lung cells by SARS-CoV-2, the virus responsible for COVID-19.

SARS-CoV-2 Mpro-IN-6 is a selective, covalent, and irreversible inhibitor of SARS-CoV-2 main protease (Mpro) with an inhibition concentration (IC50) of 0.18 μM, and does not inhibit human cathepsins B, F, K, and L, or caspase 3.

Hydroxychloroquine Impurity E, an impurity found in Hydroxychloroquine, a synthetic antimalarial compound that also inhibits Toll-like receptor 7 9 (TLR7 9) signaling, has been shown to effectively inhibit SARS-CoV-2 infection in vitro [1] [2] [3].

Hydroxychloroquine Impurity F, an impurity in Hydroxychloroquine, is identified in the synthetic antimalarial agent known for its capability to inhibit Toll-like receptor 7 9 (TLR7 9) signaling. Additionally, Hydroxychloroquine demonstrates effective inhibition of SARS-CoV-2 infection in vitro [1] [2] [3].

Imatinib Impurity E is a specific impurity found in Imatinib, an orally available inhibitor of multiple tyrosine kinases, including BCR ABL, v-Abl, PDGFR, and c-kit. Imatinib (STI571) operates by semi-competitively inhibiting enzyme activity; it binds adjacent to the ATP binding site, inducing a closed or self-inhibited conformation [1] [2] [3] [4]. Additionally, Imatinib acts as an inhibitor against SARS-CoV and MERS-CoV [5].

Desmethylazelastine, the primary active metabolite of Azelastine, undergoes oxidative metabolism via the cytochrome P450 enzyme system, exhibits a 97% protein binding rate, and has an elimination half-life of 54 hours. Azelastine, an orally active, selective, and high-affinity histamine H1-receptor antagonist, is utilized in the research of allergic rhinitis, asthma, diabetic hyperlipidemia, and SARS-CoV-2 [1] [2] [3] [4] [5].