SARS-CoV Inhibitor

Merafloxacin (CI-934), a fluoroquinolone antibacterial agent, is a selective programmed -1 ribosomal frameshifting (-1 PRF) inhibitor of beta coronaviruses. Merafloxacin exhibits in vitro activity against gram-positive and gram-negative bacteria.

Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a K_i value of 6 nM and an EC₉₀ value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 2.3 μM.

Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC₅₀ of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.

Quipazine is a 5-HT agonist with a K_i value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC₅₀ of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.

Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC₅₀s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC₅₀ of 3.1 μM), HCoV-229E (IC₅₀ of 0.7 μM) and HCoV-OC43.

Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir hydrate inhibits SARS-CoV-2 3CL^pro activity.

JNJ-9676 is an orally active Coronavirus M protein inhibitor and selective Sarbecovirus inhibitor. JNJ-9676 binds to the M protein dimer and forces the protein into an alternative conformational state with a compound-induced binding pocket. JNJ-9676 demonstrates in vitro nanomolar antiviral activity against SARS-CoV-2, SARS-CoV and Sarbecovirus strains from bat and pangolin zoonotic origin.

Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a K_i of 8.6 nM.

Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a K_i of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL^pro inhibitor.

MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC₅₀ value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells.

Debrisoquin (hydroiodide) is the hydrochloride form of Debrisoquin (HY-B1624). Debrisoquin is a TMPRSS2 inhibitors that inhibits SARS-CoV-2 entry into human lung cell line by a TMPRSS2-depedent manner. Debrisoquin can be used for antiviral research.

3’OMe-m7GpppAmpG (m7(3'OMeG)(5')ppp(5')(2'OMeA)pG) ammonium solution (100 mM) is a trinucleotide Cap1 analog with the structure m7 (3'OMeG)(5') ppp (5')(2'OMeA) pG, and also functions as a cis-acting ligase ribozyme inhibitor. 3’OMe-m7GpppAmpG ammonium solution (100 mM) effectively reduces free 5'-triphosphate groups on RNA transcripts, thereby enabling efficient co-transcriptional capping of in vitro transcribed mRNA. 3’OMe-m7GpppAmpG ammonium solution (100 mM) is not only widely used in the preparation of modified mRNA including trivalent influenza vaccine candidates, but also applicable to studies related to SARS-CoV-2 infection and other relevant research.

Aloin B (Isobarbaloin) is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC₅₀ of 16.08 μM (hydrolytic activity) and 17.51 μM (deubiquitinase activity). Aloin B is metabolized by rat intestinal flora into aloe-emodin-9-anthrone to exert laxative effects. Aloin B inhibits TPA (HY-18739)-induced ear edema, putrescine elevation, and tumor promotion in mouse skin. Aloin B can be used in research related to anti-inflammation, tumor promotion inhibition, coronavirus disease 2019 (COVID-19) and constipation.

JFD00244 is a sirtuin 2 (SIRT2) inhibitor, with anti-tumor effect. JFD00244 is also a Nsp-16 inhibitor against SARS-CoV-2.

Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-Cyclin E1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC₅₀ of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection.

Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC₅₀ values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis.

Lufotrelvir (PF-07304814), a phosphate proagent of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle.

PF-00835231 is a CoV-2 cysteine 3C-like protease (3CL^pro) inhibitor, with IC₅₀s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CL^pro, respectively. PF-00835231 is developed for the research of anti-SARS-CoV-2/COVID-19. PF-00835231 can inhibit cell infections and also suppress infections in animal models.

Dexamethasone-4,6α,21,21-d₄ is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.

HeE1-2Tyr, a pyridobenzothiazole compound, is a flavivirus RNA dependent RNA polymerases (RdRp) inhibitor. HeE1-2Tyr significantly inhibits West Nile, Dengue and SARS-CoV-2 RdRps (IC₅₀ of 27.6 μM) activity in vitro.