COVID-19

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  • COVID-19 Inhibitors (57)
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Catalog No. Product Name Information Product Use Citations Product Validations
E0052New Merafloxacin Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
S0833 EIDD-1931 EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir.
S1183 Danoprevir (ITMN-191) Danoprevir (ITMN-191, RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
Viruses, 2019, 11(11)
S1185 Ritonavir (ABT-538) Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
mBio, 2021, 12(1)e02754-20
Cell Chem Biol, 2021, S2451-9456(21)00441-4
J Antimicrob Chemother, 2021, 76(7):1874-1885
S1289 Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
Cancer Cell, 2021, S1535-6108(21)00659-0
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1322 Dexamethasone (MK-125) Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Mol Syst Biol, 2021, 17(9):e10426
Cell Rep, 2021, 36(2):109360
Cell Rep, 2021, 37(5):109912
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
S1380 Lopinavir (ABT-378) Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
mBio, 2021, 12(1)e02754-20
J Antimicrob Chemother, 2021, 76(7):1874-1885
Antiviral Res, 2021, 185:104996
S1386 Nafamostat mesilate (FUT-175) Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.
bioRxiv, 2021, 2021.03.31.437960
EMBO J, 2020, e2020106057
bioRxiv, 2020, 2020.10.02.324228
S1401 Tenofovir Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.
Antiviral Res, 2021, S0166-3542(21)00068-1
PLoS Pathog, 2020, 16(12):e1009024
Cells, 2020, 17;9(4) pii: E1003
S1538 Telaprevir (VX-950) Telaprevir (VX-950, LY-570310, MP-424) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
Cell Rep, 2021, 35(7):109133
Int J Mol Sci, 2021, 22(9)4559
Sci Rep, 2021, 11(1):19443
S1620 Darunavir Ethanolate Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
Sci Rep, 2021, 11(1):19443
Antimicrob Agents Chemother, 2020, AAC.00872-20
J Virol, 2019, 93(9)
S1680 Disulfiram (NSC 190940) Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
Int Immunopharmacol, 2022, 102:108401
Cancer Res, 2021, canres.1337.2021
Elife, 2021, 10e63810
S1691 Praziquantel Praziquantel is an anthelmintic effective against flatworms.
Parasitology, 2020, 1-11
PLoS Negl Trop Dis, 2015, 9(3):e0003593
S1706 Lamivudine (BCH-189) Lamivudine (BCH-189, GR109714X) is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase.
Front Cardiovasc Med, 2021, 8:634774
ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
Antiviral Res, 2020, 175:104709
S1759 Pitavastatin (NK-104) calcium Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancer Discov, 2021, candisc.0551.2021
Transl Oncol, 2021, 14(7):101107
S1835 Azithromycin (CP-62993) Azithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Biomolecules, 2020, 10(10)E1395
S2071 Prulifloxacin (NM441) Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
J Virol, 2021, JVI0177821
S2079 Moexipril HCl Moexipril HCl (RS-10085) is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure.
S2169 Rosuvastatin (ZD4522) calcium Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancers (Basel), 2021, 13(21)5543
Cell Death Dis, 2021, 12(1):78
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
Cancers (Basel), 2021, 13(8)1954
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Pharmacol Res, 2021, 174:105927
S2823 Tideglusib (NP031112) Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.
J Virol, 2021, JVI.02393-20
Adv Biol Regul, 2021, S2212-4926(20)30091-9
Mol Cell, 2020, 80(6):1104-1122.e9
S2851 Baricitinib (INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
Immunity, 2021, 54(11):2514-2530.e7
Mol Syst Biol, 2021, 17(9):e10426
Cell Death Dis, 2021, 12(10):864
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Cancer Cell, 2021, S1535-6108(20)30609-7
Sci Adv, 2021, 7(23)eabg2697
Autophagy, 2021, 1-14
S2874 Camostat Mesilate Camostat (FOY-305, FOY-S980) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.
Nat Commun, 2021, 12(1):866
Biomedicines, 2021, 9(4)437
bioRxiv, 2021, 2021.03.31.437960
S2926 TDZD-8 TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
Sci Transl Med, 2020, 12(554):eaba3613
FASEB J, 2018, 32(7):3924-3935
Nat Commun, 2017, 1;8(1):1232
S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Blood, 2021, 138(9):790-805
Int J Mol Sci, 2021, 22(3)1362
Sci Rep, 2021, 11(1):12148
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Cancer Cell Int, 2020, 19;20:58
S3079 Atovaquone Atovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.
Sci Rep, 2019, 9(1):536
Sci Transl Med, 2015, 7(290):290ra89
S3124 Dexamethasone Acetate Dexamethasone (NSC 39471) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Cell Rep, 2021, 36(2):109360
J Control Release, 2021, S0168-3659(21)00446-6
Mol Cancer, 2021, 20(1):84
S3511New FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
S3724 Velpatasvir Velpatasvir (GS-5816) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
Drug Metab Dispos, 2020, 48(12):1264-1270
Front Microbiol, 2020, 10:2936
S3733 Boceprevir Boceprevir (EBP 520, SCH 503034) is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1.
Cell Rep, 2021, 35(7):109133
Front Pharmacol, 2021, 12:720018
Sci Rep, 2021, 11(1):19443
S4028 Dexamethasone Sodium Phosphate Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Cell Rep, 2021, 36(2):109360
Mol Cancer, 2021, 20(1):84
JCI Insight, 2021, 6(19)e147038
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Bone, 2022, 154:116262
Cancer Cell, 2021, S1535-6108(21)00659-0
Gut, 2021, 70(5):890-899
S4282 Nelfinavir (AG 1343) Mesylate Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
Cell Rep, 2021, 35(10):109218
Protein Cell, 2021, 10.1007/s13238-021-00885-0
Sci Rep, 2021, 11(1):19443
S4430 Hydroxychloroquine Sulfate (NSC 4375) Hydroxychloroquine Sulfate (NSC 4375, HCQ) 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.
Autophagy, 2021, 1-14
EMBO Mol Med, 2021, 13(9):e13193
Cell Rep, 2021, 35(1):108940
S4646 Ciclesonide Ciclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases.
Drug Test Anal, 2020, 10.1002/dta.2917
S5250 Darunavir Darunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
Sci Rep, 2021, 11(1):19443
ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
Antimicrob Agents Chemother, 2020, AAC.00872-20
S5754 Baricitinib phosphate Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19.
J Immunother Cancer, 2021, 9(6)e002305
Front Immunol, 2021, 12:720697
J Cell Mol Med, 2021, 10.1111/jcmm.16684
S5911 Bictegravir Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
J Antimicrob Chemother, 2021, dkab276
S5940 Bepotastine Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease.
S6676 Ebselen Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay.
Viruses, 2021, 13(2)173
Antiviral Res, 2020, 182:104924
S6999New Chloroquine (NSC-187208) Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bone, 2022, 154:116262
Dev Cell, 2021, 56(16):2313-2328.e7
Autophagy, 2021, 10.1080/15548627.2021.1912270
S7262 Vidofludimus Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S7392 Loxistatin Acid (E-64C) Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry.
ACS Chem Biol, 2021, 16(9):1628-1643
Sci Signal, 2018, 11(518)eaao0422
Sci Signal, 2018, 11(518)eaao0422
S7393 Aloxistatin (E64d) Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
EMBO J, 2021, e108050
Protein Cell, 2021, 10.1007/s13238-021-00858-3
PLoS Pathog, 2021, 17(9):e1009889
S7579 Ledipasvir (GS5885) Ledipasvir (GS5885) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection.
Sci Rep, 2021, 11(1):19443
Cancers (Basel), 2019, 11(10)E1407
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
S7947 PX-12 PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.
Free Radic Biol Med, 2020, S0891-5849(20)31609-9
Exp Neurol, 2020, 329:113302
Front Pharmacol, 2020, 15;11:712
S7975 Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
mBio, 2021, 12(1)e02754-20
Antiviral Res, 2021, S0166-3542(21)00068-1
Toxicol Sci, 2021, kfab079
S8279 Shikonin (C.I. 75535) Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
J Cancer, 2021, 12(1):76-88
Cancer Sci, 2021, 112(9):3507-3519
J Cell Mol Med, 2021, 10.1111/jcmm.17007
S8932 Remdesivir (GS-5734) Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.
Nat Commun, 2021, 12(1):5553
Nat Commun, 2021, 12(1):668
EMBO J, 2021, e107826
S8969 Molnupiravir (EIDD-2801) 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.
S9567 Indinavir Sulfate Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS.
Mol Metab, 2020, 29;101027
Antimicrob Agents Chemother, 2020, AAC.00872-20
Mol Ther, 2018, 26(6):1435-1446
S9731New PF-00835231 PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.
Nat Commun, 2021, 12(1):6786
S9858New Lufotrelvir (PF-07304814)

PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.

S9866New Nirmatrelvir (PF-07321332)

Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.

E0052New Merafloxacin Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
S0833 EIDD-1931 EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir.
S1183 Danoprevir (ITMN-191) Danoprevir (ITMN-191, RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
Viruses, 2019, 11(11)
S1185 Ritonavir (ABT-538) Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
mBio, 2021, 12(1)e02754-20
Cell Chem Biol, 2021, S2451-9456(21)00441-4
J Antimicrob Chemother, 2021, 76(7):1874-1885
S1289 Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
Cancer Cell, 2021, S1535-6108(21)00659-0
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1322 Dexamethasone (MK-125) Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Mol Syst Biol, 2021, 17(9):e10426
Cell Rep, 2021, 36(2):109360
Cell Rep, 2021, 37(5):109912
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
S1380 Lopinavir (ABT-378) Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
mBio, 2021, 12(1)e02754-20
J Antimicrob Chemother, 2021, 76(7):1874-1885
Antiviral Res, 2021, 185:104996
S1386 Nafamostat mesilate (FUT-175) Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.
bioRxiv, 2021, 2021.03.31.437960
EMBO J, 2020, e2020106057
bioRxiv, 2020, 2020.10.02.324228
S1401 Tenofovir Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.
Antiviral Res, 2021, S0166-3542(21)00068-1
PLoS Pathog, 2020, 16(12):e1009024
Cells, 2020, 17;9(4) pii: E1003
S1538 Telaprevir (VX-950) Telaprevir (VX-950, LY-570310, MP-424) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
Cell Rep, 2021, 35(7):109133
Int J Mol Sci, 2021, 22(9)4559
Sci Rep, 2021, 11(1):19443
S1620 Darunavir Ethanolate Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
Sci Rep, 2021, 11(1):19443
Antimicrob Agents Chemother, 2020, AAC.00872-20
J Virol, 2019, 93(9)
S1680 Disulfiram (NSC 190940) Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
Int Immunopharmacol, 2022, 102:108401
Cancer Res, 2021, canres.1337.2021
Elife, 2021, 10e63810
S1691 Praziquantel Praziquantel is an anthelmintic effective against flatworms.
Parasitology, 2020, 1-11
PLoS Negl Trop Dis, 2015, 9(3):e0003593
S1706 Lamivudine (BCH-189) Lamivudine (BCH-189, GR109714X) is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase.
Front Cardiovasc Med, 2021, 8:634774
ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
Antiviral Res, 2020, 175:104709
S1759 Pitavastatin (NK-104) calcium Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancer Discov, 2021, candisc.0551.2021
Transl Oncol, 2021, 14(7):101107
S1835 Azithromycin (CP-62993) Azithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Biomolecules, 2020, 10(10)E1395
S2071 Prulifloxacin (NM441) Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
J Virol, 2021, JVI0177821
S2079 Moexipril HCl Moexipril HCl (RS-10085) is a potent orally active nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, used for the treatment of hypertension and congestive heart failure.
S2169 Rosuvastatin (ZD4522) calcium Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancers (Basel), 2021, 13(21)5543
Cell Death Dis, 2021, 12(1):78
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
Cancers (Basel), 2021, 13(8)1954
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Pharmacol Res, 2021, 174:105927
S2823 Tideglusib (NP031112) Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.
J Virol, 2021, JVI.02393-20
Adv Biol Regul, 2021, S2212-4926(20)30091-9
Mol Cell, 2020, 80(6):1104-1122.e9
S2851 Baricitinib (INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
Immunity, 2021, 54(11):2514-2530.e7
Mol Syst Biol, 2021, 17(9):e10426
Cell Death Dis, 2021, 12(10):864
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Cancer Cell, 2021, S1535-6108(20)30609-7
Sci Adv, 2021, 7(23)eabg2697
Autophagy, 2021, 1-14
S2874 Camostat Mesilate Camostat (FOY-305, FOY-S980) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.
Nat Commun, 2021, 12(1):866
Biomedicines, 2021, 9(4)437
bioRxiv, 2021, 2021.03.31.437960
S2926 TDZD-8 TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
Sci Transl Med, 2020, 12(554):eaba3613
FASEB J, 2018, 32(7):3924-3935
Nat Commun, 2017, 1;8(1):1232
S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Blood, 2021, 138(9):790-805
Int J Mol Sci, 2021, 22(3)1362
Sci Rep, 2021, 11(1):12148
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Cancer Cell Int, 2020, 19;20:58
S3079 Atovaquone Atovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.
Sci Rep, 2019, 9(1):536
Sci Transl Med, 2015, 7(290):290ra89
S3124 Dexamethasone Acetate Dexamethasone (NSC 39471) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Cell Rep, 2021, 36(2):109360
J Control Release, 2021, S0168-3659(21)00446-6
Mol Cancer, 2021, 20(1):84
S3511New FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
S3724 Velpatasvir Velpatasvir (GS-5816) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
Drug Metab Dispos, 2020, 48(12):1264-1270
Front Microbiol, 2020, 10:2936
S3733 Boceprevir Boceprevir (EBP 520, SCH 503034) is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1.
Cell Rep, 2021, 35(7):109133
Front Pharmacol, 2021, 12:720018
Sci Rep, 2021, 11(1):19443
S4028 Dexamethasone Sodium Phosphate Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Cell Rep, 2021, 36(2):109360
Mol Cancer, 2021, 20(1):84
JCI Insight, 2021, 6(19)e147038
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Bone, 2022, 154:116262
Cancer Cell, 2021, S1535-6108(21)00659-0
Gut, 2021, 70(5):890-899
S4282 Nelfinavir (AG 1343) Mesylate Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
Cell Rep, 2021, 35(10):109218
Protein Cell, 2021, 10.1007/s13238-021-00885-0
Sci Rep, 2021, 11(1):19443
S4430 Hydroxychloroquine Sulfate (NSC 4375) Hydroxychloroquine Sulfate (NSC 4375, HCQ) 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.
Autophagy, 2021, 1-14
EMBO Mol Med, 2021, 13(9):e13193
Cell Rep, 2021, 35(1):108940
S4646 Ciclesonide Ciclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases.
Drug Test Anal, 2020, 10.1002/dta.2917
S5250 Darunavir Darunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
Sci Rep, 2021, 11(1):19443
ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
Antimicrob Agents Chemother, 2020, AAC.00872-20
S5754 Baricitinib phosphate Baricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19.
J Immunother Cancer, 2021, 9(6)e002305
Front Immunol, 2021, 12:720697
J Cell Mol Med, 2021, 10.1111/jcmm.16684
S5911 Bictegravir Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
J Antimicrob Chemother, 2021, dkab276
S5940 Bepotastine Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease.
S6676 Ebselen Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay.
Viruses, 2021, 13(2)173
Antiviral Res, 2020, 182:104924
S6999New Chloroquine (NSC-187208) Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bone, 2022, 154:116262
Dev Cell, 2021, 56(16):2313-2328.e7
Autophagy, 2021, 10.1080/15548627.2021.1912270
S7262 Vidofludimus Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S7392 Loxistatin Acid (E-64C) Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry.
ACS Chem Biol, 2021, 16(9):1628-1643
Sci Signal, 2018, 11(518)eaao0422
Sci Signal, 2018, 11(518)eaao0422
S7393 Aloxistatin (E64d) Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
EMBO J, 2021, e108050
Protein Cell, 2021, 10.1007/s13238-021-00858-3
PLoS Pathog, 2021, 17(9):e1009889
S7579 Ledipasvir (GS5885) Ledipasvir (GS5885) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection.
Sci Rep, 2021, 11(1):19443
Cancers (Basel), 2019, 11(10)E1407
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
S7947 PX-12 PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.
Free Radic Biol Med, 2020, S0891-5849(20)31609-9
Exp Neurol, 2020, 329:113302
Front Pharmacol, 2020, 15;11:712
S7975 Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
mBio, 2021, 12(1)e02754-20
Antiviral Res, 2021, S0166-3542(21)00068-1
Toxicol Sci, 2021, kfab079
S8279 Shikonin (C.I. 75535) Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
J Cancer, 2021, 12(1):76-88
Cancer Sci, 2021, 112(9):3507-3519
J Cell Mol Med, 2021, 10.1111/jcmm.17007
S8932 Remdesivir (GS-5734) Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.
Nat Commun, 2021, 12(1):5553
Nat Commun, 2021, 12(1):668
EMBO J, 2021, e107826
S8969 Molnupiravir (EIDD-2801) 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.
S9567 Indinavir Sulfate Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS.
Mol Metab, 2020, 29;101027
Antimicrob Agents Chemother, 2020, AAC.00872-20
Mol Ther, 2018, 26(6):1435-1446
S9731New PF-00835231 PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.
Nat Commun, 2021, 12(1):6786
S9858New Lufotrelvir (PF-07304814)

PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.

S9866New Nirmatrelvir (PF-07321332)

Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.

E0052New Merafloxacin Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
S3511New FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
S6999New Chloroquine (NSC-187208) Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bone, 2022, 154:116262
Dev Cell, 2021, 56(16):2313-2328.e7
Autophagy, 2021, 10.1080/15548627.2021.1912270
S9731New PF-00835231 PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.
Nat Commun, 2021, 12(1):6786
S9858New Lufotrelvir (PF-07304814)

PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.

S9866New Nirmatrelvir (PF-07321332)

Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.