sars-cov-in-6

SARS-CoV-IN-6 (Compound 17) acts as an inhibitor of SARS-CoV-1 and SARS-CoV-2 RdRp, demonstrating an IC50 value of 7.8 μM against SARS-CoV-2 RdRp. This compound reduces the cytopathic effects of single-round infectious particles (SRIP) infected with SARS-CoV-1 and SARS-CoV-2 replicons and inhibits the expression of SARS-CoVN proteins. The EC50 values for SRIP based on SARS-CoV-1 and SARS-CoV-2 replicons are 0.12 µM and 1.47 µM, respectively.

SARS-CoV-2-IN-6 is an inhibitor of SARS-CoV-2 3CLpro with an IC50 value of 73 nM.

SARS-CoV-2 nsp13-IN-6 (compound C5) is a potent inhibitor of the SARS-CoV-2 non-structural protein 13 (nsp13), targeting ssDNA+ATPase (IC50: 27 μM) and ssDNA-ATPase (IC50: 33 μM). nsp13-IN-6 can be utilized in anti-COVID-19 research.

SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of the SARS-CoV-2 3CL protease, showing potent inhibitory activity with an IC50 of 4.9 μM, and is used in the research of coronavirus disease 2019 (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.

PLpro-IN-6 (compound 6) serves as an inhibitor for the papain-like protease (PLpro), demonstrating potent activity with an IC 50 of 0.019 μM against the SARS-CoV-2 PLpro enzyme.

SARS-CoV-2 Mpro-IN-34 (Compound 26) acts as an inhibitor of SARS-CoV-2 Mpro with an IC50 of 6 nM. It also inhibits OC43 Mpro, demonstrating an IC50 of 33 nM. Furthermore, this compound exhibits antiviral activity in Vero E6 cells infected with SARS-CoV-2, with an EC50 of 0.103 μM.

SARS-CoV-2 Mpro-IN-41 (Compound 7e) is an orally active inhibitor targeting COX-2 and SARS-CoV-2 Mpro, with respective IC50 values of 9.66 μM and 13.24 μM. It also demonstrates inhibitory activity against COX-1 (IC50: 46.11 μM). This compound significantly suppresses the expression of inflammation-related cytokines such as TNF-α, IL-6, and IL-1β, exhibiting anti-inflammatory properties. By selectively inhibiting COX-2 and SARS-CoV-2 Mpro, SARS-CoV-2 Mpro-IN-41 exerts both anti-inflammatory and antiviral effects, making it a potential candidate for research in inflammation and COVID-19 treatment.

SARS-CoV-2-IN-70 (compound 6) is an effective inhibitor of SARS-CoV-2, with an IC50 value of 3.2 μM.

PROTACSARS-CoV-2 Mpro degrader-2 (Compound 6) is a potent SARS-CoV-2 Mpro PROTAC degrader. It exhibits broad-spectrum antiviral activity against coronaviruses, including SARS-CoV-2 (EC50 = 10.8 μM), HCoV-OC43 (EC50 = 1.6 μM), and HCoV-229E (EC50 = 6.5 μM). In Calu-3 cells, it shows effective anti-SARS-CoV-2 activity with an EC50 of 0.89 μM.

F594-1001 hydrochloride (compound 6) is a potent and highly selective inhibitor of SARS-CoV-2 Mac1-ADP-ribose. It exhibits an IC50 of 8.5 μM, 68 μM, and 45 μM in AS, FP, and FRET assays against SARS-CoV-2, respectively. F594-1001 hydrochloride binds directly to SARS-CoV-2 Mac1 and inhibits Mac1 ADP-ribosylhydrolase activity in a dose-dependent manner.

SARS-CoV-2-IN-13 (compound 5) is an analogue of niclosamide, displaying greater stability in human plasma and liver S9 enzymes assay. It improves bioavailability and half-life when administered orally and is a potent SARS-CoV-2 inhibitor with an IC50 of 0.057 μM [1].

SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent inhibitor of nsp13 (non-structural protein 13), selectively inhibiting nsp13 ssDNA+ATPase with an IC50 of 6 μM, but not ssDNA-ATPase, and can be used to study COVID-19.

GRL-0820 (SARS-CoV-2-IN-6) is a potent SARS-CoV-2 3CLpro inhibitor that can be used to study novel coronavirus infections.

Ketotifen (HC 20-511) is a second-generation, orally active, noncompetitive histamine 1 (H1) receptor antagonist and mast cell stabilizer. It inhibits 6-phosphogluconate dehydrogenase (PGD) in vitro and exhibits antiviral activity against SARS-CoV-2 and the Influenza virus. Ketotifen is also used in research on autoimmune encephalomyelitis (EAE) and in the prevention of asthma attacks.

STING agonist-24 (CF504), a non-nucleotide small-molecule STING agonist, activates STING, leading to increased phosphorylation of STING, TBK1, and IRF3. It elevates levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells, demonstrating activity against SARS-CoV series strains [1].

STING agonist-23 (CF505) is a non-nucleotide, small-molecule compound that stimulates STING, enhancing the phosphorylation of STING, TBK1, and IRF3. It elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells and demonstrates efficacy against SARS-CoV strains [1].

STING agonist-23 (CF508), a non-nucleotide small-molecule STING agonist, activates STING, thereby enhancing the phosphorylation of STING, TBK1, and IRF3. This activation elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Moreover, STING agonist-23 demonstrates efficacy against SARS-CoV series strains [1].

STING agonist-23 (CF510) is a non-nucleotide, small-molecule activator of the STING pathway. It initiates the phosphorylation of STING, TBK1, and IRF3, enhancing the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Notably, it demonstrates activity against SARS-CoV series strains [1].

Clazakizumab, a monoclonal antibody, demonstrates high affinity and specificity towards the interleukin-6 (IL-6) cytokine, potentially inhibiting the cytokine response in COVID-19 caused by SARS-CoV-2. It is also under research for treating psoriatic arthritis (PsA) and renal antibody-mediated rejection [1] [2].

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].

SARS-CoV-2-IN-94 (Compound 6) exhibits antiviral activity against the COVID-19 virus by targeting the 6VSB protein (6VSB protein).

Bromhexine-d3 HCl is a deuterated compound of Bromhexine HCl. Bromhexine HCl has a CAS number of 611-75-6. Bromhexine hydrochloride is a mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus.