denv-in-2

DENV-IN-2 is a highly effective inhibitor of dengue viral replication with a potency indicated by an EC 50 of 0.016 nM. It exhibits significant activity against all four serotypes of the Dengue virus, with EC 50 values ranging from 0.013 to 0.029 nM.

A181 (AI-181) is a DENV-2 inhibitor, suitable for use in dengue fever research.

Panduratin A is a natural chalcone derivative with inhibitory activity against MMP-9 in human oral epidermoid carcinoma KB cells; inhibitory activity against the NS3 protease of DENV-2 (Ki=25 μM); significant cytotoxicity against human androgen-independent prostate cancer cells PC-3 and DU-145; and also able to activate the LKB1-AMPK- PPARα δ signaling pathway and enhance the oxidative capacity of myocyte mitochondria.

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

NS2B NS3-IN-2 is a potent, covalent inhibitor of dengue virus (DENV) NS2B NS3 with an IC50 of 6.0 nM and a Ki of 0.66 μM. It significantly increases cell viability and exhibits no cytotoxicity.

DENV-IN-10 is a potent tetravalent inhibitor of the dengue virus, with half-maximal effective concentrations (EC50s) of 1.36, 0.87, 0.94, and 0.95 μM against DENV-1, DENV-2, DENV-3, and DENV-4 serotypes, respectively. Functioning as a post-entry replication inhibitor, DENV-IN-10 demonstrates specificity for primate-origin cells [1].

DENV-IN-12 (Compound 6), a derivative of N-methylcytisine thio, effectively inhibits both DENV-1 and DENV-2. It demonstrates strong antiviral activity against DENV-2, with EC50 values between 0.002 and 0.005 μM across various cell lines [1].

NITD-2 is a dengue virus (DENV) polymerase inhibitor, inhibits the DENV RdRp-mediated RNA elongation. NITD-2 penetrates cell membrane poorly. Dengue virus (DENV) is the most prevalent mosquito- borne viral pathogen in humans. Neither vaccine nor antiviral therapy is currently available for DENV.