Imunologia e Inflamação

<p>CF504: non-nucleotide STING agonist, boosts STING, TBK1, IRF3 phosphorylation; raises IFN-β, IL-6, CXCL-10, TNF-α; active against SARS-CoV strains.</p>

<p>AChE-IN-3 had inhibitory effect on AChE and stronger inhibitory effect on NO, with EC50 of 0.57 μM.</p>

<p>Tomaralimab (OPN-305) is a humanized IgG4 monoclonal antibody targeting TLR2. Tomarlimab is used to study myelodysplastic syndromes (MDS).</p>

<p>SARS-CoV-2-IN-39 is a SARS-CoV-2 inhibitor with an EC50 of 1 μM.</p>

TMV-IN-13 (compound 5g) exhibits anti-TMV activity.

<p>NF-κB-IN-9, a nuclear factor kappa B (NF-κB) targeting sonosensitizer with excitation and emission wavelengths (λex/λem) of 489/628 nm, features dual</p>

Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.

<p>Romilkimab (SAR156597) is a chimeric humanized immunoglobulin (Ig) antibody designed to specifically target interleukins 4 and 13 (IL-4 and IL-13) [1].</p>

<p>M0324 is a MUC-1 conditional CD40 agonist composed of an anti-MUC-1 IgG and two identical CD40-targeting camelid VHH domains, selectively activate immune cells.</p>

<p>5(S),15(S)-DiHETE, made by 15-LO from 5(S)-HETE, boosts human PMNL degranulation via PAF, not fMLP/A23187/LTB4, and lures eosinophils at ED50 of 0.3μM.</p>

<p>Inflexuside A, an abietane diterpenoid from Isodon inflexus, and Inflexuside B inhibit NO in LPS-stimulated RAW264.7 cells.</p>

<p>Guignardone L, a metabolite extracted from the endophytic fungus Guignardia mangiferae, possesses toll-like receptor 3 (TLR3) regulating activity [1].</p>

<p>Cartap hydrochloride is an insecticidal derivative. It is used to control chewing and sucking insects on many crops.</p>

<p>2-Hydroxybenzylamine captures IsoLGs, prevents early atrial fibrillation recurrence post-ablation.</p>

<p>Rabelomycin is an angucycline group antibiotic.</p>

<p>Anti-inflammatory agent 64 (compound 4b) exhibits antioxidant and anti-inflammatory activities, effectively inhibiting the secretion of IL-6 and TNF-α while</p>

ISD (interferon stimulatory DNA) Control sodium is a non-immunostimulatory single-stranded oligonucleotide with a sequence identical to its double-stranded counterpart, ISD.

<p>NOX4-IN-1 (Compound 14m) is an inhibitor of NADPH oxidase 4 (NOX4) that reduces the production of reactive oxygen species (ROS). It also inhibits the TGF-β1/Smad signaling pathway, leading to decreased expression of fibrosis-related proteins. Additionally, NOX4-IN-1 impedes the migration of NRK-49F cells.</p>

<p>DEPMPO is a stable nitrone for trapping O, N, S, C radicals, used in vivo/vitro with ESR. DEPMPO-biotin tags proteins' S-nitroso groups for analysis.</p>

<p>Croconazole exhibited dose-dependent inhibitory activity on the 5-lipoxygenase (5-LOX) of neutrophils.</p>

<p>Nemolizumab (CIM331) is an anti-IL-31 receptor A monoclonal antibody for atopic dermatitis and pruritus study.</p>

<p>AMY-101 TFA is an inhibitor of complement C3 and an immunomodulator, gingivitis and periodontitis. reduces inflammation and lowers levels of MMP-8 and MMP-9</p>

Eupenicisirenin C (compound 1), a sirenin derivative, exhibits strong NF-κB inhibitory activities and suppresses the cGAS-STING pathway. Additionally, Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells [1].

<p>NLRP3-IN-66 (example 257) is a potent inhibitor of the NLRP3 inflammasome.</p>

<p>AB-680: potent, reversible CD73 inhibitor, Ki=4.9 pM, &gt;10,000-fold selectivity vs CD39, anti-tumor.</p>

<p>TLR8 agonist 2 hydrochloride: potent for human TLR8 (EC50 3 nM), weak for TLR7 (EC50 33.33 μM).</p>

<p>Diplacol, a geranylated flavanone isolated from Paulownia trees (Paulownia coreana UYEKI), exhibits anti-inflammatory properties by inhibiting NO production in LPS-stimulated Raw264.7 cells with an IC50 value of 4.53 μM [1].</p>

<p>4-Chlorochalcone is achalcone inhibit human MAO-B and ROS/RNS production and is able to inhibit the growth of CAL51 cells.</p>

FSL-1 TFA activates TLR2/6, boosts HSV-2 defense, and triggers MMP-9 via TLR2, NF-κB/AP-1 in THP-1 cells.

<p>Anti-inflammatory agent 58 exhibits IL-1β inhibition with an IC50 value of 1.08 μM and suppresses pro-inflammatory gene expression, protein secretion, and NF-κB</p>

IRBP (1-20), human is a 20-amino acid fragment of a 140-kDa glycoprotein in the retinal interphotoreceptor matrix.

<p>STING agonist-13 boosts cancer immunity by activating STING pathway, reducing tumors, and enhancing immune memory.</p>

<p>KTX-497, an IRAK4 degrader, demonstrates a potent DC50 value of 3 nM. It is utilized in oncology research[1].</p>

<p>Amaroswerin, a secoiridoid glucoside, has anti-inflammatory, antidiabetic, and other medicinal properties; it inhibits NO release at IC50 of 5.42 μg/mL.</p>

<p>NLRP3-IN-65 (compound 41) is a potent inhibitor of NLRP3.</p>

<p>R1-ICR-5 is a selective PROTAC degrader targeting serine/threonine-protein kinase 1 (RIPK1). Mediated by VHL, R1-ICR-5 promotes the degradation of RIPK1, disrupting the TNFR1 and TLR3/4 signaling hubs, enhancing NF-κB, MAPK, and IFN signal output, and facilitating RIPK3 activation and necroptosis induction. R1-ICR-5 holds potential for research in cancer and inflammatory diseases.</p>

An analog of PEP-19 with enhanced binding to and antagonism of calmodulin.

<p>BCL6 PROTAC 1: Selective BCL6 degrader, IC50 8.8 µM, used in DLBCL research.</p>

<p>MUC1: Type I transmembrane glycoprotein, overexpressed and abnormally glycosylated in cancer, binds ICAM-1 domain 1.</p>

<p>TMV-IN-6 (Compound 4g) serves as a novel antiviral and fungicidal agent that impedes tobacco mosaic virus (TMV) assembly, functioning by attachment to TMV coat</p>

<p>QKY-613 is a prodrug designed to enhance immune surveillance by targeting nucleic acid modification pathways. It selectively facilitates the incorporation of 6mdA (N6-methyl-deoxyadenosine) into viral DNA, boosting the DNA's phase separation potential and subsequently increasing cGAS activation levels to strengthen host immune surveillance. In mouse models of viral infection, QKY-613 significantly reduced mortality in aged mice. This compound holds promise for studying immune surveillance mechanisms based on nucleic acid modifications.</p>

<p>PROTAC IRAK4 degrader-2 reduces IRAK4 in PBMCs with a DC50 of 36 nM and inhibits cytokines.</p>

Anti-Mesothelin Antibody (YP218) is a chimeric rabbit IgG antibody that targets human Mesothelin.

<p>NLRP3-IN-64 (Compound 2) is an inhibitor of NLRP3, effectively suppressing its activation with an EC50 of 5 nM.</p>

<p>DHR 6G, nonfluorescent reduced Rhodamine 6G, permeates cells, indicating ROS by oxidizing to fluorescent form in mitochondria.</p>

<p>UT-11: potent, brain-permeable mPGES-1 inhibitor. IC50: 0.10μM (human SK-N-AS), 2.00μM (murine BV2). Stops PGE2 production.</p>

<p>COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX.</p>

<p>(6R)-6-Tert-butyl-10-(3-methoxypropoxy)-dihydro-2-oxo-indazole carboxylic acid has antiviral and antibacterial properties, useful for Hepatitis B research.</p>

Se-DOPE is a selenium-containing phospholipid molecule utilized for the synthesis of bifunctional Janus lipase. It facilitates the production of ROS under light induction and scavenges ROS in the presence of glutathione. Se-DOPE plays a role in regulating redox and immune homeostasis, aiding in the healing of infectious diabetic wounds.

<p>OVA Peptide(257-264) is an ovalbumin octamer Peptide expressed by class I MHC molecule h-2kb.</p>