HIV Protease Inhibitor

Escin IA is an oral LOXL2 inhibitor and EMT inhibitor, with selectivity for LOXL2-expressing cells. Escin IA suppresses invasion, migration, and metastasis of breast cancer cells, and acts as the primary anti-TNBC metastasis constituent of Aesculus chinensis Bunge fruit saponin fraction. Escin IA can be used for the research of triple-negative breast cancer, acute inflammation, and ethanol-induced gastric mucosal lesions.

Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC₅₀=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.

Hinokinin (Compound 1) is a compound isolated from the stems of Hypoestes aristate. Hinokinin exhibits moderate activity of HIV-1 protease enzyme.

Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC₅₀: 170 μM).

Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a K_i of 1 nM for wild type HIV-1 protease.

Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection.

Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.

CL-197 is an orally active and long-acting purine anti-HIV nucleoside reverse transcriptase inhibitor (NRTI). CL-197 has potential effect on the research of viral, oncological and cerebrovascular diseases. CL-197 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Ganoderic acid H is a hydroxylated lanostane-type triterpenoid derived from Ganoderma lucidum with anticancer activity. Ganoderic acid H inhibits the constitutive transactivation activity of AP-1 and NF-κB; it also downregulates the secretion of uPA and the expression of CDK4, and suppresses the growth, adhesion, migration and invasion of cancer cells. Ganoderic acid H inhibits HIV-1 protease in vitro. Ganoderic acid H can be used in studies related to breast cancer and HIV infection.

DPC-681 (DPH-153893) is an orally active HIV inhibitor. DPC-681 inhibits HIV protease activity and inhibits wild-type and mutant HIV replication. DPC-681 can be used for the research of HIV infection.

Ethyl salvianolate A (Ethyl salvionolate A) is an anti-HIV-1 compound that can be extracted from the roots of Salvia yunnanensis. Ethyl salvianolate A inhibits P24 antigen in HIV-1 infected MT-4 cell cultures (EC₅₀: 1.44 μg/mL). Ethyl salvianolate A inhibits HIV-1 replicative enzymes, with IC₅₀s of 56.38 μM (Reverse transcriptase), 12.03 μM (Protease), 14.54 μM (Integrase), respectively.

TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC₅₀ values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.

Darunavir-d9 (TMC114-d9) is the deuterium labeled Darunavir. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC₅₀ = 0.003 μM; IC₉₀ = 0.009 μM) with minimal cytotoxicity.

Isoescin IA is a triterpenoid saponin isolated from the seeds of Aesculus chinensis. Isoescin IA has anti-HIV-1 protease activity.

Telinavir (SC-52151) is a potent and selective HIV protease inhibitor. Telinavir inhibits lymphotropic, monocytotropic strains and field isolates of HIV type 1 (HIV-1), HIV-2, and simian immunodeficiency virus with EC₅₀s of 26 ng/mL (43 nM). Telinavir is highly protein bound in human plasma and exhibits low partitioning into erythrocytes.

RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC₅₀ is 54 μM) and VHR (IC₅₀ is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC₅₀s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24.

Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum.Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity. Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC₅₀ of 90 μM. Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC₅₀ of 41.7μM.

(Rac)-Telinavir ((Rac)-SC-52151) is a racemate of Telinavir (HY-106395A). Telinavir (SC-52151) is a potent and selective HIV protease inhibitor. Telinavir inhibits lymphotropic, monocytotropic strains and field isolates of HIV type 1 (HIV-1), HIV-2, and simian immunodeficiency virus with EC₅₀s of 26 ng/mL (43 nM). Telinavir is highly protein bound in human plasma and exhibits low partitioning into erythrocytes.

Ritonavir (Standard) is the analytical standard of Ritonavir. This product is intended for research and analytical applications. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.61 μM.

2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells.