COVID-19

COVID-19 Products

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  • COVID-19 Inhibitors (64)
  • New COVID-19 Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
J Transl Med, 2024, 22(1):208
iScience, 2024, 27(2):109015.
Cell Discov, 2023, 9(1):47
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).
Nat Commun, 2024, 15(1):1642
Sci Rep, 2024, 14(1):4000
Cell Discov, 2023, 9(1):92
S6999 Chloroquine Chloroquine 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.
Bioact Mater, 2024, 32:277-291
Cancer Lett, 2024, 586:216695
Basic Res Cardiol, 2024, 119(1):113-131
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) 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.
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
PLoS Pathog, 2024, 20(1):e1011958
Kidney Int, 2023, 104(5):943-955
S1322 Dexamethasone Dexamethasone 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.
Cell Host Microbe, 2024, S1931-3128(24)00005-2
Oncogene, 2024, 43(4):235-247
bioRxiv, 2024, 2024.01.29.577409
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.
Int J Mol Sci, 2024, 24;25(3):1427.
Nature, 2023, 613(7944):558-564
Cell, 2023, 186(4):850-863.e16
S3035 Daunorubicin HCl Daunorubicin HCl 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.
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
Int J Mol Sci, 2023, 24(16)12926
Cancers (Basel), 2023, 15(12)3112
S2851 Baricitinib Baricitinib 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.
Sci Rep, 2024, 14(1):4125
Nat Cancer, 2023, 4(7):984-1000
Nat Cancer, 2023, 4(7):984-1000
S2485 Mitoxantrone 2HCl Mitoxantrone 2HCl 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.
Mol Metab, 2024, 80:101873
Cell Commun Signal, 2023, 21(1):167
Int J Mol Sci, 2023, 10.3390/ijms242216375
S1380 Lopinavir (ABT-378) Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Nat Commun, 2023, 14(1):5034
Nat Commun, 2023, 14(1):5034
Int J Mol Sci, 2023, 24(7)6062
S1538 Telaprevir Telaprevir is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
J Virol, 2024, e0192123.
bioRxiv, 2023, 2023.11.22.568224
NPJ Digit Med, 2022, 5(1):83
S1185 Ritonavir Ritonavir 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.
Cancer Drug Resist, 2024, 7:3
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
Int J Mol Sci, 2023, 24(7)6062
S1680 Disulfiram Disulfiram 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).
Cell Death Dis, 2023, 14(12):825
J Transl Med, 2023, 21(1):334
Neural Regen Res, 2023, 18(2):357-363
S3124 Dexamethasone Acetate Dexamethasone (NSC 39471,Dexamethasone 21-acetate) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
STAR Protoc, 2023, 4(2):102342
Exp Mol Med, 2022, 54(9):1450-1460
iScience, 2022, 25(12):105682
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%.
Anim Nutr, 2024, 20:16:409-421.
Cell, 2023, 186(4):850-863.e16
BMC Vet Res, 2023, 19(1):60
S8279 Shikonin Shikonin, 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 Pharm Anal, 2023, 13(2):187-200
Cancer Sci, 2023, 114(3):806-821
Cancers (Basel), 2023, 15(17)4356
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.
Pharmaceutics, 2022, 14(2)400
Front Oncol, 2022, 12:888695
Sci Rep, 2022, 12(1):10616
S1401 Tenofovir Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.
Hepatol Commun, 2024, 8(1)e0351
Nat Commun, 2023, 14(1):199
Antimicrob Agents Chemother, 2023, 67(7):e0046223
S2823 Tideglusib Tideglusib 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.
SLAS Discov, 2024, S2472-5552(24)00007-8
Cell, 2022, 185(22):4135-4152.e22
Int J Mol Med, 2022, 49(6)84
S1835 Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Sci Rep, 2023, 13(1):14453
Sci Rep, 2023, 13(1):14453
J Pers Med, 2022, 12(2)258
S1759 Pitavastatin calcium Pitavastatin calcium, 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.
bioRxiv, 2024, 2024.02.02.578510
bioRxiv, 2024, 10.1101/2024.01.16.575899
Nat Commun, 2023, 14(1):3251
S7975 Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
J Med Virol, 2024, 96(1):e29372
Nat Commun, 2022, 13(1):2256
Nucleic Acids Res, 2022, gkac512
S4282 Nelfinavir Mesylate Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Int J Mol Sci, 2023, 24(7)6062
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
mBio, 2022, 13(1):e0304421
S1183 Danoprevir Danoprevir 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.
Viruses, 2023, 15(4)981
Cell Rep Methods, 2023, 3(10):100599
J Cell Biochem, 2022, 10.1002/jcb.30213
S1706 Lamivudine Lamivudine 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.
Antiviral Res, 2023, 211:105552
Hepatol Commun, 2023, 7(5)e0078
Antimicrob Agents Chemother, 2023, 67(7):e0046223
S1351 Ivermectin Ivermectin 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.
Life Sci Alliance, 2023, 6(8)e202302133
Cell Rep Methods, 2023, 3(10):100599
Front Pharmacol, 2022, 13:934746
S1289 Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
JCI Insight, 2023, 8(9)e166850
Cell Death Discov, 2023, 9(1):451
Int J Mol Sci, 2023, 24(7)6062
S1386 Nafamostat mesilate (FUT-175) Nafamostat mesilate 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.
Cell Death Dis, 2024, 15(2):109
Pathogens, 2023, 13(1)18
Nat Commun, 2022, 13(1):4804
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.
Physiol Rep, 2023, 11(19):e15829
Physiol Rep, 2023, 11(19):e15829
Inflamm Regen, 2023, 43(1):44
S2169 Rosuvastatin calcium Rosuvastatin calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.
bioRxiv, 2024, 10.1101/2024.01.16.575899
Neuron, 2023, S0896-6273(23)00513-5
Int J Mol Sci, 2023, 24(9)8359
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.
Elife, 2022, 11e77444
Antiviral Res, 2022, 202:105325
Front Microbiol, 2022, 13:884034
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.
Theranostics, 2023, 13(14):4730-4744
Theranostics, 2023, 13(14):4730-4744
CNS Neurosci Ther, 2023, 10.1111/cns.14433
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.
Eur J Med Chem, 2024, 268:116202
Antiviral Res, 2022, 204:105350
Molecules, 2022, 27(13)4292
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
J Cell Biochem, 2022, 10.1002/jcb.30213
S1620 Darunavir Ethanolate Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
J Virol, 2022, JVI0173021
J Cell Biochem, 2022, 10.1002/jcb.30213
Sci Rep, 2021, 11(1):19443
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.
Int J Mol Sci, 2023, 24(17)13593
PLoS One, 2023, 18(4):e0284332
J Cell Mol Med, 2022, 26(14):3965-3976
S5250 Darunavir Darunavir (TMC114,DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
PNAS Nexus, 2024, 3(1):pgad446
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
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.
Cell, 2023, 186(4):850-863.e16
Nat Commun, 2023, 14(1):199
Elife, 2022, 11e74443
S9866 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.

Int J Mol Sci, 2023, 24(7)6062
Antiviral Res, 2022, 203:105343
Commun Biol, 2022, 5(1):976
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
S3079 Atovaquone Atovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.
iScience, 2024, 27(3):109172
J Cell Biochem, 2022, 10.1002/jcb.30213
Elife, 2020, 9e56773
S0833 EIDD-1931 (NHC) EIDD-1931 (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.
Nucleic Acids Res, 2023, 10.1093/nar/gkad1002
NPJ Digit Med, 2022, 5(1):83
J Med Virol, 2022, 10.1002/jmv.27650
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.
Evid Based Complement Alternat Med, 2023, 2023:8378581
Science, 2022, 375(6586):1254-1261
NPJ Digit Med, 2022, 5(1):83
S4646 Ciclesonide Ciclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases.
Am J Physiol Lung Cell Mol Physiol, 2023, 324(5):L722-L736
mBio, 2022, 13(1):e0304421
Pharmaceutics, 2022, 14(7)1511
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.
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
Mol Metab, 2020, 29;101027
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
S5911 Bictegravir Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
PNAS Nexus, 2024, 3(1):pgad446
Cells, 2022, 11(11)1841
Int J Mol Sci, 2022, 23(23)15380
S9731 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.
Mol Cell, 2022, S1097-2765(22)00433-6
Bioorg Med Chem Lett, 2022, 66:128732
Nat Commun, 2021, 12(1):6786
S3724 Velpatasvir Velpatasvir (GS-5816,VEL) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
mBio, 2023, 10.1128/mbio.01318-23
Front Oncol, 2021, 11:803278
Front Microbiol, 2020, 10:2936
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.
Int J Mol Sci, 2023, 24(4)4235
J Med Virol, 2022, 10.1002/jmv.27891
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S1691 Praziquantel Praziquantel is an anthelmintic effective against flatworms.
Parasitology, 2020, 1-11
PLoS Negl Trop Dis, 2015, 9(3):e0003593
S2071 Prulifloxacin (NM441) Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
J Cell Biochem, 2022, 10.1002/jcb.30213
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.
J Cell Biochem, 2022, 10.1002/jcb.30213
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.
J Cell Biochem, 2022, 10.1002/jcb.30213
S9858 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.

S3511 FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
E3896 Perilla Leaf Extract Perilla Leaf Extract is extracted from the leaves of Perilla frutescens, which is capable of inhibiting SARS-CoV-2 replication by inactivating the virion.
S0875 XP-59 XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM.
E1112 GS-621763 GS-621763, an orally bioavailable prodrug of GS-441524, shows a dose-dependent antiviral effect on SARS-CoV-2 reporter virus expressing nanoluciferase (SARS-CoV-2 nLUC) replication with an EC50 of 2.8 μM, also inhibits reporter SARS-CoV-2 expressing firefly luciferase (SARS-CoV-2 Fluc) replication with EC50 of 0.125 μM. 
S3553 Riamilovir Riamilovir (Triazavirin) is a broad-spectrum antiviral drug candidate, which can be used for potential application against the Coronavirus 2019-nCoV.
E1111 VV116 VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM.
E0052 Merafloxacin Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
E1131 Ensitrelvir fumarate S-217622 (Ensitrelvir fumarate) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor with IC50 of 13 nM.
S9963 paquinimod Paquinimod (ABR 25757), a specific inhibitor of S100A8/A9, could rescue the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice.
E1174 Coronastat(NK01-63) Coronastat(NK01-63) is a potent inhibitor of the SARS-CoV-2 3CL protease, which is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle.
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.
J Transl Med, 2024, 22(1):208
iScience, 2024, 27(2):109015.
Cell Discov, 2023, 9(1):47
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).
Nat Commun, 2024, 15(1):1642
Sci Rep, 2024, 14(1):4000
Cell Discov, 2023, 9(1):92
S6999 Chloroquine Chloroquine 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.
Bioact Mater, 2024, 32:277-291
Cancer Lett, 2024, 586:216695
Basic Res Cardiol, 2024, 119(1):113-131
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) 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.
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
PLoS Pathog, 2024, 20(1):e1011958
Kidney Int, 2023, 104(5):943-955
S1322 Dexamethasone Dexamethasone 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.
Cell Host Microbe, 2024, S1931-3128(24)00005-2
Oncogene, 2024, 43(4):235-247
bioRxiv, 2024, 2024.01.29.577409
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.
Int J Mol Sci, 2024, 24;25(3):1427.
Nature, 2023, 613(7944):558-564
Cell, 2023, 186(4):850-863.e16
S3035 Daunorubicin HCl Daunorubicin HCl 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.
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
Int J Mol Sci, 2023, 24(16)12926
Cancers (Basel), 2023, 15(12)3112
S2851 Baricitinib Baricitinib 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.
Sci Rep, 2024, 14(1):4125
Nat Cancer, 2023, 4(7):984-1000
Nat Cancer, 2023, 4(7):984-1000
S2485 Mitoxantrone 2HCl Mitoxantrone 2HCl 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.
Mol Metab, 2024, 80:101873
Cell Commun Signal, 2023, 21(1):167
Int J Mol Sci, 2023, 10.3390/ijms242216375
S1380 Lopinavir (ABT-378) Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Nat Commun, 2023, 14(1):5034
Nat Commun, 2023, 14(1):5034
Int J Mol Sci, 2023, 24(7)6062
S1538 Telaprevir Telaprevir is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
J Virol, 2024, e0192123.
bioRxiv, 2023, 2023.11.22.568224
NPJ Digit Med, 2022, 5(1):83
S1185 Ritonavir Ritonavir 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.
Cancer Drug Resist, 2024, 7:3
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
Int J Mol Sci, 2023, 24(7)6062
S1680 Disulfiram Disulfiram 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).
Cell Death Dis, 2023, 14(12):825
J Transl Med, 2023, 21(1):334
Neural Regen Res, 2023, 18(2):357-363
S3124 Dexamethasone Acetate Dexamethasone (NSC 39471,Dexamethasone 21-acetate) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
STAR Protoc, 2023, 4(2):102342
Exp Mol Med, 2022, 54(9):1450-1460
iScience, 2022, 25(12):105682
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%.
Anim Nutr, 2024, 20:16:409-421.
Cell, 2023, 186(4):850-863.e16
BMC Vet Res, 2023, 19(1):60
S8279 Shikonin Shikonin, 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 Pharm Anal, 2023, 13(2):187-200
Cancer Sci, 2023, 114(3):806-821
Cancers (Basel), 2023, 15(17)4356
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.
Pharmaceutics, 2022, 14(2)400
Front Oncol, 2022, 12:888695
Sci Rep, 2022, 12(1):10616
S1401 Tenofovir Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.
Hepatol Commun, 2024, 8(1)e0351
Nat Commun, 2023, 14(1):199
Antimicrob Agents Chemother, 2023, 67(7):e0046223
S2823 Tideglusib Tideglusib 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.
SLAS Discov, 2024, S2472-5552(24)00007-8
Cell, 2022, 185(22):4135-4152.e22
Int J Mol Med, 2022, 49(6)84
S1835 Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Sci Rep, 2023, 13(1):14453
Sci Rep, 2023, 13(1):14453
J Pers Med, 2022, 12(2)258
S1759 Pitavastatin calcium Pitavastatin calcium, 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.
bioRxiv, 2024, 2024.02.02.578510
bioRxiv, 2024, 10.1101/2024.01.16.575899
Nat Commun, 2023, 14(1):3251
S7975 Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
J Med Virol, 2024, 96(1):e29372
Nat Commun, 2022, 13(1):2256
Nucleic Acids Res, 2022, gkac512
S4282 Nelfinavir Mesylate Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Int J Mol Sci, 2023, 24(7)6062
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
mBio, 2022, 13(1):e0304421
S1183 Danoprevir Danoprevir 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.
Viruses, 2023, 15(4)981
Cell Rep Methods, 2023, 3(10):100599
J Cell Biochem, 2022, 10.1002/jcb.30213
S1706 Lamivudine Lamivudine 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.
Antiviral Res, 2023, 211:105552
Hepatol Commun, 2023, 7(5)e0078
Antimicrob Agents Chemother, 2023, 67(7):e0046223
S1351 Ivermectin Ivermectin 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.
Life Sci Alliance, 2023, 6(8)e202302133
Cell Rep Methods, 2023, 3(10):100599
Front Pharmacol, 2022, 13:934746
S1289 Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
JCI Insight, 2023, 8(9)e166850
Cell Death Discov, 2023, 9(1):451
Int J Mol Sci, 2023, 24(7)6062
S1386 Nafamostat mesilate (FUT-175) Nafamostat mesilate 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.
Cell Death Dis, 2024, 15(2):109
Pathogens, 2023, 13(1)18
Nat Commun, 2022, 13(1):4804
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.
Physiol Rep, 2023, 11(19):e15829
Physiol Rep, 2023, 11(19):e15829
Inflamm Regen, 2023, 43(1):44
S2169 Rosuvastatin calcium Rosuvastatin calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.
bioRxiv, 2024, 10.1101/2024.01.16.575899
Neuron, 2023, S0896-6273(23)00513-5
Int J Mol Sci, 2023, 24(9)8359
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.
Elife, 2022, 11e77444
Antiviral Res, 2022, 202:105325
Front Microbiol, 2022, 13:884034
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.
Theranostics, 2023, 13(14):4730-4744
Theranostics, 2023, 13(14):4730-4744
CNS Neurosci Ther, 2023, 10.1111/cns.14433
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.
Eur J Med Chem, 2024, 268:116202
Antiviral Res, 2022, 204:105350
Molecules, 2022, 27(13)4292
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
J Cell Biochem, 2022, 10.1002/jcb.30213
S1620 Darunavir Ethanolate Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
J Virol, 2022, JVI0173021
J Cell Biochem, 2022, 10.1002/jcb.30213
Sci Rep, 2021, 11(1):19443
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.
Int J Mol Sci, 2023, 24(17)13593
PLoS One, 2023, 18(4):e0284332
J Cell Mol Med, 2022, 26(14):3965-3976
S5250 Darunavir Darunavir (TMC114,DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
PNAS Nexus, 2024, 3(1):pgad446
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
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.
Cell, 2023, 186(4):850-863.e16
Nat Commun, 2023, 14(1):199
Elife, 2022, 11e74443
S9866 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.

Int J Mol Sci, 2023, 24(7)6062
Antiviral Res, 2022, 203:105343
Commun Biol, 2022, 5(1):976
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
S3079 Atovaquone Atovaquone (Atavaquone) is a medication used to treat or prevent for pneumocystis pneumonia, toxoplasmosis, malaria, and babesia.
iScience, 2024, 27(3):109172
J Cell Biochem, 2022, 10.1002/jcb.30213
Elife, 2020, 9e56773
S0833 EIDD-1931 (NHC) EIDD-1931 (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.
Nucleic Acids Res, 2023, 10.1093/nar/gkad1002
NPJ Digit Med, 2022, 5(1):83
J Med Virol, 2022, 10.1002/jmv.27650
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.
Evid Based Complement Alternat Med, 2023, 2023:8378581
Science, 2022, 375(6586):1254-1261
NPJ Digit Med, 2022, 5(1):83
S4646 Ciclesonide Ciclesonide (Alvesco, Omnaris, RPR251526, Zetonna) is a glucocorticoid used to treat obstructive airway diseases.
Am J Physiol Lung Cell Mol Physiol, 2023, 324(5):L722-L736
mBio, 2022, 13(1):e0304421
Pharmaceutics, 2022, 14(7)1511
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.
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
Mol Metab, 2020, 29;101027
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
S5911 Bictegravir Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
PNAS Nexus, 2024, 3(1):pgad446
Cells, 2022, 11(11)1841
Int J Mol Sci, 2022, 23(23)15380
S9731 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.
Mol Cell, 2022, S1097-2765(22)00433-6
Bioorg Med Chem Lett, 2022, 66:128732
Nat Commun, 2021, 12(1):6786
S3724 Velpatasvir Velpatasvir (GS-5816,VEL) is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
mBio, 2023, 10.1128/mbio.01318-23
Front Oncol, 2021, 11:803278
Front Microbiol, 2020, 10:2936
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.
Int J Mol Sci, 2023, 24(4)4235
J Med Virol, 2022, 10.1002/jmv.27891
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S1691 Praziquantel Praziquantel is an anthelmintic effective against flatworms.
Parasitology, 2020, 1-11
PLoS Negl Trop Dis, 2015, 9(3):e0003593
S2071 Prulifloxacin (NM441) Prulifloxacin (NM441, AF 3013), the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent.
J Cell Biochem, 2022, 10.1002/jcb.30213
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.
J Cell Biochem, 2022, 10.1002/jcb.30213
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.
J Cell Biochem, 2022, 10.1002/jcb.30213
S9858 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.

S3511 FOY251 FOY251, an active metabolite of camostat mesilate, is an inhibitor of synthetic serine protease. FOY251 inhibits SARS-CoV-2 infection.
E3896 Perilla Leaf Extract Perilla Leaf Extract is extracted from the leaves of Perilla frutescens, which is capable of inhibiting SARS-CoV-2 replication by inactivating the virion.
S0875 XP-59 XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM.
E1112 GS-621763 GS-621763, an orally bioavailable prodrug of GS-441524, shows a dose-dependent antiviral effect on SARS-CoV-2 reporter virus expressing nanoluciferase (SARS-CoV-2 nLUC) replication with an EC50 of 2.8 μM, also inhibits reporter SARS-CoV-2 expressing firefly luciferase (SARS-CoV-2 Fluc) replication with EC50 of 0.125 μM. 
E1111 VV116 VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM.
E0052 Merafloxacin Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses.
E1131 Ensitrelvir fumarate S-217622 (Ensitrelvir fumarate) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor with IC50 of 13 nM.
S9963 paquinimod Paquinimod (ABR 25757), a specific inhibitor of S100A8/A9, could rescue the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice.
E1174 Coronastat(NK01-63) Coronastat(NK01-63) is a potent inhibitor of the SARS-CoV-2 3CL protease, which is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle.

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