HIV Inhibitor

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.

Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer.

Limonin inhibits HIV-1 with an EC₅₀ of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC₅₀ of 54.74 μM. Limonin has antiviral and antitumor activities.

Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.

Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC₅₀ value of 13 nM against CXCR4 ¹²⁵I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC₅₀ of 1 and 9 nM, respectively.Mavorixafor trihydrochloride can be used for the study of WHIM syndrome.

1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC₅₀ of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor. 1-Deoxymannojirimycin hydrochloride has antiviral activity against HIV‐1 strains . 1-Deoxymannojirimycin hydrochloride increases high mannose structures. 1-Deoxymannojirimycin hydrochloride can be used for the study of liver cancer and colon cancer.

Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC₅₀s of 30, 170, 100 nM, respectively.

5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na⁺/H⁺ exchanger inhibitor, which decreases the intracellular pH (pH_i) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC₅₀s of 3.91 μM and 1.34 μM, respectively.

Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (K_i=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg²⁺ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection.

Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.

Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (K_i=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.

Dextran sulfate sodium salt (DSS) (MW 4500-5500) is a polymer of dehydrated glucose with a molecular weight of approximately 4500-5500. Dextran sulfate sodium salt with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 4500-5500) is an inhibitor of complement and coagulation pathways, and belongs to the glycosaminoglycans (GAG) family. Dextran sulfate sodium salt (MW 4500-5500) acts as an anticoagulant, antiviral, and anti-lipemic agent. Dextran sulfate sodium salt (MW 4500-5500) stops HIV-1 virus adsorption to host cells. Dextran sulfate sodium salt (MW 4500-5500) prevents NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 4500-5500) inhibits instant blood-mediated inflammatory reaction (IBMIR).

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC₅₀ of 2.1 nM.

BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC₅₀ of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with K_i of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.

Anti-Mouse/Rat/Human CCL2/MCP-1 Antibody (2H5) is an anti-mouse/rat/human CCL2/MCP-1 IgG monoclonal antibody. Anti-Mouse/Rat/Human CCL2/MCP-1 Antibody (2H5) can reverse the immunosuppressive microenvironment by blocking the CCL2 signaling pathway. Anti-Mouse/Rat/Human CCL2/MCP-1 Antibody (2H5) can reduce the secretion of IFN-γ and the infiltration of macrophages. CCL2/MCP-1 Antibody (2H5) can reduce the amount of HIV virus by increasing the proportion of T cells. Anti-Mouse/Rat/Human CCL2/MCP-1 Antibody (2H5) can be used for researches on inflammation conditions, virus infection and cancer such as inflammatory bowel disease (IBD), hepatocellular carcinoma (HCC) and HIV.

Trigonelline chloride is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline chloride is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline chloride also has anti-HSV-1, antibacterial, and antifungal activity, and induces ferroptosis.

Berberrubine chloride is an orally active metabolite of berberine. Berberrubine chloride alleviates mucosal lesions and inflammation in mouse colitis models. Berberrubine chloride has anti-inflammatory, anti-tumor, and antiviral activities.

Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC₅₀ of 130 nM, and 0.02-0.46 μM, respectively.

Ditiocarb sodium (Sodium diethyldithiocarbamate) is an orally active copper reagent. Ditiocarb sodium exhibits activities such as antioxidation, chelation, anti-tumor effects, immunomodulation, and anti-HIV properties. Ditiocarb sodium can be used in the research of tumors, inflammatory, and immune-related diseases.

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