Protein Tyrosine Kinases

Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.

Imatinib mesylate, a selective tyrosine kinase inhibitor, induced a sustained objective response in treating gastrointestinal stromal tumors with the inhibition of the KIT signal-transduction pathway.

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.

Emodin is a purgative resin, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). It belongs to a family of compounds called anthraquinones, which have shown anti-inflammatory and anticancer effects

Methylprednisolone is an apoptosis inducer and was also found to inhibit human small cell lung cancer cell growth in vitro.

KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.

Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.

Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist.

Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.

Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.

NPI64 is a broad-spectrum coronavirus protease inhibitor which inhibits viral 3C and 3C-like protease.

Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile.

Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.

LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).

Auranofin is a gold salt classified by the World Health Organization as an antirheumatic agent. It is a gold-thiol complex with anti-inflammatory and immunosuppressive actions.

Paquinimod is a S100A9 inhibitor, which prevents S100A9 binding to TLR-4.

Galidesivir hydrochloride (BCX 4430 hydrochloride) is a viral RNA-dependent RNA polymerase (RdRp) inhibitor; demonstrated broad-spectrum activity in multiple viruses and a favorable preliminary preclinical safety profile.

Artefenomel (OZ439) is a synthetic antimalarial agent with the artemisinin pharmacophore. Artefenomel (OZ439) is a long-acting artemisinin-related agent.

GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM.

XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM.

Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19.

FOY 251, an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor. FOY 251 inhibits SARS-CoV-2 infection in cells assay.

Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation.

Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities.

Merafloxacin, also known as CI 934, is a fluoroquinolone antibacterial, which was also identified as a -1 PRF inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on -1 PRF of other beta coronaviruses. Importantly, frameshift inhibition by merafloxacin substantially impedes SARS-CoV-2 replication in Vero E6 cells, thereby providing the proof of principle of targeting -1 PRF as an effective antiviral strategy for SARS-CoV-2.

AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.