Factor B-IN-1

Factor B-IN-1 is a Factor B inhibitor (IC50 = 43 nM) and is an analog of compound 13. It is used to inhibit complement pathway factor B and has improved pharmacokinetic properties (oral availability in rats and dogs).

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).

CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C

Gramicidin A is a peptide antibiotic isolated from B. brevis.Gramicidin A is a highly hydrophobic channel-forming ion carrier that forms monovalent cation-permeable channels in artificial membranes.Gramicidin A induces the degradation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) and reduces the growth of a mouse xenograft model of human renal cell carcinoma. Gramicidin A has antibacterial, antimalarial and hemolytic activities.

(±)8-HEPE is produced by the non-enzymatic oxidation of EPA, containing equal amounts of 8(S)-HEPE and 8(R)-HEPE. The ability of (±)8-HEPE to induce hatching of E. modestus and B. balanoides eggs is probably due to the presence of the 8(R) isomer within the racemic mixture.[1][2]

STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR).References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018). STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α/β receptor (IFNAR). References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018).

Lavendustin B is a Tyrosine Kinase Inhibitor and an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF p75).

Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

Factor B-IN-4 is a potent inhibitor (IC50: 1 μM) of complement factor B. Factor B-IN-4 can be used to study inflammatory and immune-related diseases.

1. Ruscogenin has anti-inflammatory activity, suppressed zymosan A-evoked peritoneal total leukocyte migration in mice in a dose-dependent manner, 2. Ruscogenin inhibited adhesion of leukocytes to a human umbilical vein endothelial cell line (ECV34) injured by tumor necrosis factor-alpha (TNF-alpha) in a concentration-dependent manner. 3. Ruscogenin significantly attenuate LPS-induced acute lung injury via inhibiting expressions of TF and iNOS and NF-kappa B p65 activation.

MptpB-IN-1 is a potent, orally active MptpB inhibitor that targets the Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB), a secreted virulence factor evading host antimicrobial mechanisms. It effectively diminishes the survival and infection burden of multidrug-resistant Mycobacterium tuberculosis.

Dehydrobruceine B, a quassinoid isolated from Brucea javanica, demonstrates a synergistic effect with Cisplatin in inducing apoptosis through the mitochondrial pathway. It enhances the expression of apoptosis-inducing factor (AIF) and Bax while inhibiting Keap1-Nrf2 [1].

S961 acetate is a selective and high-affinity antagonist of the insulin receptor (IR), demonstrating IC50 values of 0.048 nM for HIR-A, 0.027 nM for HIR-B, and 630 nM for the human insulin-like growth factor I receptor (HIGF-IR) in SPA assays [1].

Vosoritide (BMN 111), a modified recombinant C-type natriuretic peptide (CNP) analogue, engages with natriuretic peptide receptor type B (NPR-B) to diminish the function of fibroblast growth factor receptor 3 (FGFR3). This compound is employed in the study of achondroplasia and dwarfism [1] [2] [3].

Befovacimab (BAY 1093884), a fully human monoclonal IgG2 antibody, binds to the tissue factor pathway inhibitor (TFPI). It is utilized in research for haemophilia A B [1].

Tifcemalimab (JS004), a humanized monoclonal antibody targeting BTLA (B and T lymphocyte attenuation factor), inhibits the HVEM-BTLA interaction by binding to BTLA. This action prevents the BTLA-mediated inhibitory signaling pathway, making Tifcemalimab a potential tool in cancer research [1].

Nonacog alfa (BAX326), a recombinant human factor IX, is utilized in the study of hemophilia B [1].

Dalcinonacog alfa, a recombinant factor IX (FIX), is utilized in the research of Hemophilia B [1].

Cyclo(CLLFVY) is an inhibitor of hypoxia-inducible factor-1 (HIF-1), exhibiting half-maximal inhibitory concentrations (IC50) of 19 μM in U2OS cells and 16 μM in MCF-7 cells. It binds to the PAS-B domain of HIF-1α, inhibiting the dimerization and transcriptional activity of HIF-1. Moreover, cyclo(CLLFVY) downregulates the expression of hypoxia response genes (such as VEGF and CAIX), demonstrating antitumor effects against HIF-1-related cancers.

1. Kamebakaurin (Kamebakaurine) has the ability to protect the liver from APAP-induced hepatotoxicity, presumably by both inhibiting the inflammatory response and oxidative stress. 2. Kamebakaurin inhibits the expression of hypoxia-inducible factor-1α and its target genes to confer antitumor activity. 3. Kamebakaurin has anti-cancer and anti-inflammatory activities through direct inhibition of DNA-binding activity of nuclear factor-kappa B (NF-κB) p50.4. Kamebakaurin has anti-neuroinflammatory activity via inhibition of c-Jun NH -terminal kinase and p38 mitogen-activated protein kinase pathway in activated microglial cells.