COVID-19 Compound Repurposing

COVID-19 is a potentially fatal respiratory disease caused by a strain of coronavirus, termed SARS-CoV-2. In humans, coronaviruses cause respiratory tract infections with symptoms ranging from mild, similar to the common cold, to severe pneumonia-like symptoms, as is seen with SARS (severe acute respiratory syndrome), MERS (Middle East respiratory syndrome) and COVID-19.

Tocris products are for biomedical research use only. They are not intended for human or veterinary use.

Products
Background
Literature (1)
Cat. No. Product Name / Activity
6960 ABT 199
Exhibits binding to SARS-CoV-2 Mpro in a virtual screen; selective and high affinity Bcl-2 inhibitor;
4274 AP 24534
Identified as targeting human proteins in the SARS-CoV-2 interactome; potent multi-kinase and pan-Bcr-Abl inhibitor
7283 Apilimod dimesylate
Inhibits cellular entry by SARVS-CoV-2 S pseudovirions; potent and selective PIKfyve inhibitor
4139 Aprotinin
Inhibits SARS-CoV-2 infection in vitro; serine protease inhibitor
7235 Arbidol
Inhibits replication of SARS-CoV-2 in vitro; broad spectrum antiviral
6358 Atovaquone
Exhibits anti-MERS-CoV activity in vitro; DHODH inhibitor
4600 Auranofin
Inhibits SARS-CoV-2 infection in vitro
3771 Azithromycin
Predicted to disrupt binding of SARS-CoV-2 spike protein to ACE2.
7222 Baricitinib
In silico modelling predicts inhibition of SARS-CoV-2 cell entry; highly potent JAK inhibitor
3193 Camostat mesylate
Inhibits entry of SARS-Cov-2 into lung cells; protease inhibitor
4455 Captopril
Targets human proteins in the SARS-CoV-2 interactome; ACE inhibitor
4109 Chloroquine diphosphate
Inhibits SARS-CoV-2 infection in vitro
6357 Ciclesonide
Inhibits replication fo SARS-CoV-2 in vitro; glucocorticoid
1364 Colchicine
Identified as a candidate for repurposing for COVID-19
0970 Cycloheximide
Exhibits anti-MERS-CoV activity in vitro; protein synthesis inhibitor
1101 Cyclosporin A
Inhibits coronavirus replication; cyclophilin inhibitor
7223 Dabrafenib mesylate
Targets human proteins in the SARS-CoV-2 interactome; potent and selective B-Raf, CDK16 and NEK9 inhibitor
6710 Darunavir
Predicted to bind PLpro of SARS-CoV-2; potent HIV protease inhibitor
6793 Dasatinib
Inhibits replication of SARS-CoV and MERS-CoV in vitro; thioredoxin reductase inhibitor
1467 Daunorubicin hydrochloride
Identified as targeting human proteins in the SARS-CoV-2 interactome; DNA topoisomerase II inhibitor
1126 Dexamethasone
Anti-inflammatory glucocorticoid
4583 Digoxin
Exhibits anti-MERS-CoV activity in vitro; Na+/K+ ATPase inhibitor
3807 Disulfiram
SARS-CoV-2 Mpro inhibitor; also reversibly stimulates SERCA Ca2+-ATPase
5245 Ebselen
Inhibits SARS-CoV-2 Mpro in vitro
7290 Famotidine
Inhibits histamine-induced mast cell activation; potent H2 receptor inverse agonist
3631 FK 506
Identified as targeting human proteins in the SARS-CoV-2 interactome; potent calcineurin inhibitor
3259 Gemcitabine hydrochloride
Inhibits replication of coronaviruses; DNA synthesis inhibitor
7227 GS 441524
Viral RNA-dependent RNA polymerase inhibitor; exhibits antiviral activity against SARS-CoV-2 in vitro
0931 Haloperidol hydrochloride
Targets human proteins in the SARS-CoV-2 interactome
5648 Hydroxychloroquine sulfate
Inhibits SARS-CoV-2 viral infection in vitro
5906 Imatinib mesylate
Inhibits replication of SARS-CoV and MERS-CoV in vitro; potent and selective v-Abl tyrosine kinase inhibitor
1708 Indomethacin
Identified as targeting human proteins in the SARS-CoV-2 interactome
1260 Ivermectin
Inhibits replication of SARS-Cov-2 in vitro; antiparasitic and antiviral
2959 Lercanidipine hydrochloride
Exhibits anti-MERS-CoV activity in vitro; CaV1.x blocker
3765 Linezolid
Identified as targeting human proteins in the SARS-CoV-2 interactome; antibiotic
0840 Loperamide hydrochloride
Inhibits replication of coronaviruses in vitro; peripherally acting μ opioid agonist and Ca2+ channel blocker
7052 Lopinavir
Inhibits SARS-CoV-2 replication in vitro; highly potent and selective HIV-1 protease inhibitor
3798 Losartan potassium
Reduces lung injury in a mouse model of SARS-CoV infection; Selective AT1 antagonist
2874 Luteolin
Binds SARS-CoV-2 Mpro in molecular docking studies; also also anti-inflammatory, antioxidant and free radical scavenger
6819 Mefloquine hydrochloride
Exhibits antiviral activities against SARS-CoV-2; also Cx36 and Cx50 gap channel blocker
2864 Metformin hydrochloride
Identified as targeting human proteins in the SARS-CoV-2 interactome
3081 Nafamostat mesylate
Inhibits SARS-CoV-2 infection in vitro; serine protease inhibitor
3766 Nelfinavir mesylate
Exhibits anti-MERS-CoV activity in vitro; potent HIV-1 protease inhibitor
2583 Omeprazole
Enhances anti-SARS-CoV-2 activity of serine protease inhibitors
1076 Ouabain
Exhibits anti-MERS-CoV activity in vitro; Na+/K+ ATPase inhibitor
2992 PKC 412
Identified as targeting human proteins in the SARS-CoV-2 interactome
1125 Quercetin
Inhibits SARS-CoV Mpro; also non-selective PI 3-kinase inhibitor
1292 Rapamycin
Inhibits MERS-CoV infection; mTOR inhibitor and immunosuppressant
7226 Remdesivir
Viral RNA-dependent RNA polymerase inhibitor; exhibits antiviral activity against SARS-CoV-2 in vitro
4501 Ribavirin
Inhibits cytopathic effect of SARS-CoV in vitro; guanosine analog and IMPDH inhibitor
5856 Ritonavir
Improves outcome in an animal model of MERS-CoV infection; HIV protease inhibitor
7064 Ruxolitinib
Targets human proteins in the SARS-CoV-2 interactome; potent and selective JAK1/JAK2 inhibitor
4418 Saquinavir mesylate
Modeling predicts inhibitor action at SARS-CoV-2 Mpro; HIV protease inhibitor
7189 Saracatinib
Inhibits replication of MERS-CoV and other coronaviruses; Src tyrosine kinase family inhibitor; orally bioavailable
3784 Sildenafil citrate
Reduces pulmonary pressure and edema; potent PDE5 inhibitor; orally active
0652 Thalidomide
Predicted to reduce cytokine release in SARS-CoV-2 infection; inhibits synthesis of TNF-α
2815 Valproic acid, sodium salt
Identified as targeting human proteins in the SARS-CoV-2 interactome
0654 Verapamil hydrochloride
Targets human proteins in the SARS-CoV-2 interactome; CaV1.x blocker
7187 Zanamivir
Potent influenza virus neuraminidase inhibitor;

COVID-19 is a form of severe acute respiratory syndrome (SARS) that emerged in the city of Wuhan, China, in 2019. The disease results from infection with a coronavirus known as SARS-CoV-2, which enters the lower respiratory system causing viral pneumonia; it may also affect the gastrointestinal system, heart, kidney, liver, and central nervous system leading to multiple organ failure.

Coronaviruses are enveloped, positive-sense single-stranded RNA viruses encapsulated within a nucleocapsid having helical symmetry. SARS-CoV-2 is closely related to another coronavirus responsible for a previous outbreak of SARS in 2003 (approximately 80% identity). The causative agents of the two SARS outbreaks, as well as an outbreak of Middle East respiratory syndrome (MERS) in 2012, are members of a subgroup of coronaviruses known as betacoronaviruses. The viral genome of betacoronaviruses encodes more than 20 proteins, some of which show promise as antiviral targets.

Among the viral proteins being investigated as potential therapeutic targets are two proteases: SARS coronavirus main proteinase (also known as 3C-like protease or 3CLpro) and papain-like protease, (PLpro) both of which are essential for virus replication. These proteases cleave the two translated polyproteins, PP1A and PP1AB, into functional proteins. SARS-CoV and SARS-CoV-2 3CLpro gene sequences have approximately 96% homology.

The host protease angiotensin converting enzyme 2 (ACE2) is also being investigated as a potential target for COVID-19 therapies. ACE2 is highly expressed in lung alveolar cells and high expression levels are also seen in glandular cells, endothelial cells, and enterocytes in the gastrointestinal system. The spike (S) protein is a structural protein on the outside of the nucleocapsid of coronaviruses. The virus is able to enter the host cell by binding of the S protein to ACE2 on the cell surface. Another host protein, the protease TMPRSS2 is also essential for host cell invasion, by activating the S protein and enhancing cell entry by SARS-CoV-2.

Repurposing existing therapies is an approach being widely investigated to discover treatments for COVID-19. Screening compound libraries, such as the Tocriscreen library of FDA approved drugs (Cat. No. 7200), for their activity against known viral or host targets could aid the rapid discovery of products that can prevent/treat the infection or alleviate symptoms in patients. In addition to repurposing existing medicines, technologies have emerged with the potential to aid coronavirus research and the diagnosis of COVID-19, such as Light-Up Aptamer Systems. Read more in this article from GEN.

Literature for COVID-19 Compound Repurposing

Tocris offers the following scientific literature for COVID-19 Compound Repurposing to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Coronavirus Research Brochure

Coronavirus Research Brochure eBook

COVID-19 is a potentially fatal form of pneumonia that emerged in China in 2019. It is caused by a newly identified coronavirus termed SARS-CoV-2. This brochure provides an overview of our knowledge of the virus and highlights products available from Bio-Techne to enable research into finding a treatment, including:

  • Antibodies, Recombinant Proteins, Small Molecules
  • Immunoassays
  • Cell Isolation and Identification Kits
  • Tocriscreen Compound Libraries
  • RNAscopeTM Assays
  • Instrumentation