Virus Protease

Rupintrivirvr (AG7088) is a selective rhinovirus (HRV) 3C cysteine protease mimetic peptide inhibitor with antiviral and immunomodulatory activities.Rupintrivirvr inhibits the replication of EV71 and EV-D68, and may be useful for the study of viral infections.

Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.

Theaflavin 3,3'-digallate, a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines.

Dynasore (Dynamin Inhibitor I), a cell-permeable chemical, can reversibly and non-competitivity inhibit GTPase activity of dynamin 1 2 (IC50: 15 μM in a cell-free assay). It also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase.

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1 2 3 6 7 11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

alpha-Mangostin (Mangostin) is a natural xanthonoid, a type of organic compound isolated from various parts of the mangosteen tree.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+ K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Brequinar (NSC-368390) is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.

DB772 is a broad-spectrum antiviral activity that inhibits Bovine Viral Diarrhea Virus (BVDV), prion activity, Border Disease Virus (BDV), HoBi Virus, Forked Horn Virus and Bungowannah Virus.

Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5 210 μg mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities.

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

1. Genkwanin (Apigenin 7-methyl ether) exerts its anti-inflammatory effect mainly through the regulation of the miR-11 MKP-1 MAPK pathway. 2. Genkwanin is transported by both passive diffusion and multidrug resistance protein (MDR)-mediated efflux mechanisms.

Cephaeline hydrochloride, a phenolic alkaloid found in Indian Ipecac, effectively inhibits the infection of viruses ZIKV and EBOV.

Trachelogenin ((-)-Trachelogenin), isolated from Combretum fruticosum, is an HCV entry inhibitor with anti-proliferative effects. Its mechanism is related to affecting the phosphorylation of key proteins such as β-Catenin, c-Myc and GSK3 in the β-Catenin signaling pathway. chemical and concentration-dependent. Trachelogenin has antiviral, anti-inflammatory and analgesic activities with IC50 of 0.325 and 0.259 μg mL in HCVcc and HCVpp models, respectively.

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

Lirilumab (IPH2102) is an antibody against the lethal immunoglobulin-like receptor antibody KIR2D with antitumor activity that enhances the anti-HPV + cervical cancer activity of natural killer cells through VAV1-dependent NF-κB deinhibition. It can be used to study leukemia, head and neck squamous cell carcinoma (SCCHN).

4-Phenylbutyric acid (Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and an endoplasmic reticulum stress (ERS) inhibitor. 4-Phenylbutyric acid can be used to treat urea cycle disorders.

NIOCH 14 is an orally available antiviral compound that inhibits external keratovirus, poxvirus, and smallpox virus.

Glycyrrhizic acid (Glycyrrhizin) is a triterpenoid saponinl with anti-tumor and anti-diabetic activities.

Retro-2 cycl is a dihydroquinazolinone (DHQZ) retrograde trafficking inhibitor. Retro-2 cycl (RN 1-001) inhibits JCPyV and HPV16 pseudovirus(IC50s of 54 μM and 160 μM, respectively),with antiviral agent.

Tin-protoporphyrin IX dichloride (SnPPIX dichloride) is an HO-1) inhibitor with antiviral activity that inhibits dengue and yellow fever viruses.

Novobiocin is an orally active and potent antibiotic.Novobiocin is a DNA gyrase inhibitor and heat shock protein 90 (Hsp90) antagonist with inhibitory effects on gyrase and Hsp90. Novobiocin has anti-positive activity and can be used to study highly resistant pneumococcal infections.

Lanatoside C (Ceglunate) is a cardiac glycoside, a type of drug that can be used in the treatment of congestive heart failure and cardiac arrhythmia (irregular heartbeat). Lanatoside C can be used orally or by the intravenous route.

L-Lysine-13C6-15N2 Hydrochloride is L-Lysine hydrochloride labeled with 13C and 15N isotopes. L-Lysine hydrochloride is an essential amino acid for humans and a common food additive. It stimulates the secretion of pepsin and gastric acid, enhances gastric juice secretion, and promotes growth and development in children.

Norwogonin (5,7,8-Trihydroxyflavone), isolated from Scutellaria baicalensis Georgi, possesses antiviral activity against Enterovirus 71 (IC50: 31.83 μg ml).

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP LIP CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562 ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K Akt NF-κB pathway, and probably served as a most promising agent for CML treatment.

FGI-106 tetrahydrochloride demonstrates potent inhibitory activity across a broad spectrum of viruses, including those causing hemorrhagic fevers such as Ebola, Rift Valley, and Dengue Fever, with half-maximal effective concentrations (EC50s) of 100 nM, 800 nM, and 400-900 nM, respectively. Additionally, it effectively inhibits non-hemorrhagic fever viruses, notably HCV and HIV-1, with EC50s of 200 nM and 150 nM, respectively, indicating its broad-spectrum antiviral potential.

A2ti-1 is a highly selective inhibitor of annexin A2 S100A10 heterotetramer (A2t) (IC50: 24 μM) that inhibits ARV-mediated activation of Src and p38 mitogen-activated protein kinase (MAPK). A2ti-1 can be used to study human papillomavirus type 16 (HPV16) infection.

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

AZ960 is an effective ATP competitive JAK2 inhibitor (IC50 Ki: <3 nM and0.45 nM).

A2ti-2 is a low affinity and selective inhibitor of the membrane-bound protein A2 S100A10 heterotetramer (A2t) (IC50 : 230 μM).A2ti-2 exhibits antiviral activity by selectively disrupting protein interactions between A2 and S100A10, and protects against human papillomavirus type 16 (HPV16) infection.

(+)-JNJ-A07 is a pan-serotypic dengue virus inhibitor that targets NS3-NS4B interaction with high potency. (+)-JNJ-A07 has antiviral activity and can be used to study dengue virus infections.

Denv-in-5 is an effective and selective dengue virus (DENV) inhibitor with EC50 values of 1.47, 9.23, 7.08, 8.91 μM for denV-I-IV and 0.1512 μM for HIV-1IIIB.

NGI-1 (ML414) is a cell-permeable inhibitor of oligosaccharyltransferase (OST) that can effectively reduce virus infectivity without affecting cell viability.

ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.

Andecaliximab is a recombinant IgG4 monoclonal antibody targeting matrix metalloproteinase 9 (MMP9). Andecaliximab showed antifibrotic effects in a mouse model of idiopathic pulmonary fibrosis. Andecaliximab can be used to study gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF), as well as dengue virus.

LHF-535 is an antiviral compound. It has EC50s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.

Hinokitiol (4-Isopropyltropolone) can inhibit ultraviolet B-induced apoptosis in keratinocytes and strongly suggest that the inhibitory mechanism is due to the antioxidant activity of metallothionein induced by the agent. Also, Hinokitiol modulates estrogen receptor signaling and inhibits proliferation of human breast cancer cells.

L-Lysine (Aminutrin) is one of nine essential amino acids in humans required for growth and tissue repair, Lysine is supplied by many foods, especially red meats, fish, and dairy products. Lysine seems to be active against herpes simplex viruses and present in many forms of diet supplements. The mechanism underlying this effect is based on the viral need for amino acid arginine; lysine competes with arginine for absorption and entry into cells. Lysine inhibits HSV growth by knocking out arginine.

3-Deazaneplanocin A (DZNep) is a dual inhibitor of histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (AHCY) with antipoxidative activity that inhibits hepatic, renal, peritoneal, and airway fibrosis by inducing proteasomal degradation of its targets and reducing toxicity in animal models.

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

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).

STING agonist-1 (G10) is a human-specific agent that elicits antiviral activity against emerging Alphaviruses.

SRPIN340 (SRPK inhibitor), a serine arginine-rich protein kinase (SRPK)-specific inhibitor, is potent for SRPK1 (IC50 = 0.89 uM).

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

MOSLOFLAVONE showed promising anti-inflammatory activity via inhibition of TNF-α and IL-1β with IC50 values of 0.71 μM and 7.8 μM, respectively.