Virus Protease Inhibitor

L-Lysine-¹⁵N-1 (dihydrochloride) is the ¹⁵N-labeled L-Lysine. L-lysine is an essential amino acid with important roles in connective tissues and carnitine synthesis, energy production, growth in children, and maintenance of immune functions.

NS2B/NS3-IN-4 (Compound 34e) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC₅₀ values of 0.69 µM and 1.04 µM against DENV2 and ZIKV NS2B/NS3 proteases, respectively.

NS2B/NS3-IN-6 (Compound 1a) is an allosteric DENV and ZIKV NS2B/NS3 protease inhibitor with IC₅₀ values of 2.23 µM and 25.2 µM against ZIKV and DENV proteases, respectively.

SARS-CoV-2 Mpro-IN-44 (Compound 25) is a broad-spectrum coronavirus main protease (Mpro) inhibitor. SARS-CoV-2 Mpro-IN-44 has inhibitory activity against a variety of high-risk coronaviruses (including SARS-CoV-2 and PEDV, etc.) (IC₅₀: < 0.6 μM). SARS-CoV-2 Mpro-IN-44 achieves broad-spectrum inhibition of coronaviruses by enhancing the interaction with the conserved sites of Mpro. SARS-CoV-2 Mpro-IN-44 can be used for anti-coronavirus drug development.

Abz-Nle-Lys-Arg-Arg-Ser-3-(NO2)Tyr is a WNV NS2B-NS3 protease substrate. Abz-Nle-Lys-Arg-Arg-Ser-3-(NO2)Tyr is used for WNV NS2B-NS3 protease substrate peptide selective inhibitor development.

Antiviral agent 54 (compound 33) is a broad-spectrum and orally active antiviral agent. Antiviral agent 54 shows antiviral activity for ZIKV, HCoV-OC43 and influenza A virus (IVA). Antiviral agent 54 decreases the ZIKV RNA and protein level.

FL-166 is a SARS coronavirus main protease (Mpro) inhibitor (K_i: 40 nM). FL-166 exerts its inhibitory effect by targeting a cluster of serine residues near the active site of the protease. FL-166 can be used in the study of SARS-CoV.

SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of Main Protease (M^Pro) and Cathepsin L (CatL), with IC₅₀s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC₅₀ value of 8.2 nM.

HCVcc-IN-1 is a benzothiazole-2-thiophene S-glycoside derivative with low toxic and antiviral activity.

Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC₅₀s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouse plasma stability, and no obvious cytotoxicity.

TMP1 is an orally active bispecific inhibitor of M pro (IC₅₀ = 312.5 nM)/TMPRSS2 (IC₅₀ = 1.28 μM, K_D = 10.10 μM). TMP1 exhibits broad protection against different SARS-CoV-2 variants in vitro. TMP1 cross-protects against highly pathogenic coronaviruses (SARS-CoV-1, SARS-CoV-2, and MERS-CoV) in vivo and effectively blocks the transmission of SARS-CoV-2. TMP1 can inhibit infection by SARS-CoV-2 escape mutants that are resistant to Nivolumab (HY-P9903). TMP1 can be used in coronavirus research.

FGA145 is a dual, selective inhibitor for M^pro and human Cathepsin L, with K_is of 3.71 μM, 9.82 μM and 53 nM, for Mal-M^pro, pET21-M^pro and Cathepsin L, respectively. FGA145 reveals a multitarget effects in the antiviral activity.

JMX0254 is an orally active and potent inhibitor of the dengue virus NS4B protein. JMX0254’s EC₅₀ for DENV-1, DENV-2, and DENV-3 are 0.78 µM, 0.16 µM, and 0.035 µM, respectively. JMX0254 can be used for research on viral infections.

L-Lysine-¹³C₆,¹⁵N₂,d₉ (dihydrochloride) is the deuterium, ¹³C-, and 15-labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.

cTEV6-2 binds to the cysteine residue (C151) of tobacco etch virus protease (TEV protease), and covalently inhibits TEV protease with an IC₅₀ of 81.7 nM.

UCI-1 is a SARS-CoV-2 main protease (M^pro) cyclic peptide inhibitor with an IC₅₀ of 160 μM. UCI-1 shows no obvious cytotoxicity at the concentration of inhibiting M^pro. UCI-1 can be used in the study of anti-COVID-19 drugs.

Dutacatib is inhibitor for SARS-CoV-2 3CL^pro and cathepsin K, which exhibits antiviral activity and ameliorates the cancer-induced bone diseases.

SARS-CoV-2-IN-58 (Compound 21H) is an antiviral agent against SARS-CoV-2 (EC₅₀: 18 μM). SARS-CoV-2-IN-58 inhibits SARS-CoV-2 M^pro with an IC₅₀ of 0.35 μM.

CYP2C9/CYP2C19-IN-1 (compound 22d) is a potent CYP2C9/CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C9/CYP2C19-IN-1 can be used in study of anti-ZIKV.

ZIKV-IN-4 (compound 5b) is a low-cytotoxicity and acid-stable anti-ZIKV agent (EC₅₀=3.49 μM). ZIKV-IN-4 effectively inhibits the activity of ZIKV NS5 MTase.