Immunology and Inflammation

<p>DCFBC is a low-molecular-weight radiotracer. It targets prostate-specific membrane antigen (PSMA).</p>

<p>Redaporfin (F-2BMet, LUZ-11) is a PDT cancer photosensitizer; 83% of mice had tumor regression with 1.5 mg/kg and 74 J/cm² light.</p>

<p>hSTING activator-1 (Compound 68) is a STING agonist capable of effectively activating various human STING variants (R232, H232, HAQ), with EC50 values of 56 nM, 89 nM, and 51 nM, respectively. This compound activates the type I interferon pathway by directly binding to the STING protein and stabilizing its conformation, which leads to downstream IRF3 phosphorylation and cytokine release. hSTING activator-1 also demonstrates potential in cancer research by inhibiting fibrosarcoma tumor growth.</p>

<p>Neuroprotective agent 5 (compound 28) acts as a brain-penetrating agent with anti-neuroinflammatory, antioxidant, and neuroprotective properties. It exhibits potent inhibition of nitric oxide (NO) with an EC50 of 0.49 μM and suppresses the release of pro-inflammatory mediators PGE2 and TNF-α. Additionally, it downregulates the expression of iNOS and COX-2 proteins, facilitating the polarization of BV-2 cells from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype. Neuroprotective agent 5 also dose-dependently inhibits acetylcholinesterase (AChE) activity and the aggregation of Aβ42. This compound is useful for research into Alzheimer's disease.</p>

<p>PF-06342674 is a humanized monoclonal antibody targeting the IL-7 receptor-α, with immunoregulatory activity, used in Type 1 diabetes research.</p>

<p>NLRP3-IN-73 (W16) is an orally bioavailable inhibitor that disrupts the assembly of the NLRP3 inflammasome, exhibiting an IC50 value of 0.18 μM for the NLRP3/IL-1β pathway.</p>

<p>Biotin-labeled ODN TTAGGG (sodium) is an inhibitory oligonucleotide (ODN) that functions as an antagonist to TLR9, AIM2, and cGAS.</p>

<p>SARS-CoV-2 Mpro-IN-41 (Compound 7e) is an orally active inhibitor targeting COX-2 and SARS-CoV-2 Mpro, with respective IC50 values of 9.66 μM and 13.24 μM. It also demonstrates inhibitory activity against COX-1 (IC50: 46.11 μM). This compound significantly suppresses the expression of inflammation-related cytokines such as TNF-α, IL-6, and IL-1β, exhibiting anti-inflammatory properties. By selectively inhibiting COX-2 and SARS-CoV-2 Mpro, SARS-CoV-2 Mpro-IN-41 exerts both anti-inflammatory and antiviral effects, making it a potential candidate for research in inflammation and COVID-19 treatment.</p>

<p>GHN105 is an orally active STING inhibitor that suppresses STING-dependent IFN-β secretion in THP-1 human monocytes with an IC50 of 4.4 μM. In mice, GHN105 reduces serum levels of IFN-β, IL-6, and CXCL10, and alleviates colitis in a DSS-induced acute colitis mouse model. Additionally, GHN105 demonstrates favorable pharmacokinetic properties in mice, with an oral bioavailability of 43% and a half-life of 1.1 hours.</p>

<p>CD19 CAR circRNA expresses a CD19 car protein for CAR-T immunotherapy targeting B-cell antigens.</p>

<p>TSR-033 is a human IgG4 antibody with high affinity for LAG-3 (lymphocyte activation gene-3), a co-receptor linked to diminished T cell activity, frequently co-</p>

<p>Fentiazac (BR-700) is an oral NSAID for pain, inflammation, fever, studied for arthritis and tendonitis.</p>

<p>Prifelone (R 830) is a non-steroidal anti-inflammatory compound with antioxidant activity.</p>

<p>RH-EDA, a rhodamine-based turn-on fluorescent probe, detects hydroxyl radicals ([OH]) in living systems.</p>

<p>MC4762 is an inhibitor of NOX2 and MAOB, with IC50 values of 0.155 μM and 0.182 μM, respectively. It exhibits anti-inflammatory properties by suppressing the production of ROS and downregulating the expression of pro-inflammatory cytokines such as iNOS, IL-1β, and IL-6.</p>

<p>STING ligand-4 (Compound 2) is a nitro-free covalent STING inhibitor with an IC50 of less than 0.2 μM. It can be utilized in the synthesis of PROTACSTINGdegrader-4.</p>

<p>α-Glucosidase/NLRP3-IN-1 (Compound 8) acts as a dual inhibitor targeting both α-glucosidase and NLRP3. It features an IC50 value of 6.6 μM for α-glucosidase and inhibits NLRP3 across multiple cell lines at a concentration of 100 μM. This compound demonstrates neuroprotective and antidiabetic properties, making it suitable for related research.</p>

<p>Eblasakimab (ASLAN004) is a humanized monoclonal antibody targeting IL-13α, which blocks IL-4 and IL-13 signaling through the type II receptor.</p>

<p>AMG 108 (MEDI 8968) is a fully human monoclonal antibody targeting IL-1R1, used in rheumatoid arthritis research.</p>

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

<p>N(G)-Nitroarginine-4-nitroanilide is an anti-nociceptive in mice.</p>

<p>Amfenac is a nonsteroidal anti-inflammatory drug. Amfenac also has acetic acid moiety.</p>

<p>Aβ-IN-6 is an orally active compound exhibiting anti-inflammatory, antioxidant, and anti-oligomeric activities, with significant implications for Alzheimer's</p>

<p>Perfluorododecanoic acid (PFDoA) is a PFAS pollutant causing ROS increase, mitochondrial damage, and neuronal cytotoxicity.</p>

<p>DA-E 5090, an active metabolite of E 5090, inhibits IL-1 production in human monocytes.</p>

<p>PSMA-ALB-56: radioactive, PSMA-targeted ligand, antitumor, combines glutamic urea, DOTA, albumin, with iodophenyl or tolyl fragments.</p>

<p>RS 09 TFA is a TLR4 agonist and LPS peptide analogue, promotes NF-κB nuclear translocation, induces inflammatory cytokine secretion in RAW264.7 macrophages.</p>

<p>Varokibart (TEV-53275) is a human IgG4λ antibody that targets interleukin-5 (IL-5) [1].</p>

<p>4-HNE, a marker of oxidative stress, arises from oxidized ω-6 fats like linoleic acid and shows cytotoxic and genotoxic effects.</p>

<p>BMS-986148 is a CHO-expressed humanized antibody-drug coupling targeting mesothelin-expressing cells for cytotoxic load delivery.</p>

<p>Zuberitamab (HS006) is a monoclonal antibody targeting CD20, utilized in cancer research, notably in diffuse large B-cell lymphoma [1].</p>

<p>Lonazolac Calcium, a nonsteroidal anti-inflammatory drug (NSAID), is used to treat inflammation and pain.</p>

<p>Schisanchinin D is a useful organic compound for research related to life sciences. The catalog number is T125682 and the CAS number is 1614245-13-4.</p>

<p>PSMA-D5 exhibits a binding affinity for PSMA with a Ki of 0.21 nM and becomes useful for PSMA tracing following radiolabeling. When marked with [68Ga], PSMA-D5 contains a DOTA chelator, facilitating the convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. Additionally, [68Ga]-labeled PSMA-D5 demonstrates exceptional pharmacokinetic properties and significant tumor uptake in 22Rv1 tumors. This compound can be employed in the synthesis and research of radiolabeled conjugates (RDC).</p>

<p>DZ-837 is a PROTAC that targets the BCL6 protein. The composition of DZ-837 includes the BCL6 ligand-2, the E3 ubiquitin ligase ligand Thalidomide-4-OH, and a PROTAC Linker. The configuration notably features a conjugate of the E3 ubiquitin ligase ligand and the Linker, designated as 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione.</p>

<p>4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole.</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>

<p>Axinelline A: COX inhibitor, IC50 of 2.22 μM (COX-2) &amp; 8.89 μM (COX-1), anti-inflammatory.</p>

<p>Compound 2, an N-acetyldopamine dimer from Periostracum Cicadae, exhibits antioxidant and anti-inflammatory properties.</p>

<p>Biotin-labeled Agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist, facilitates the assessment of cellular uptake and localization of</p>

<p>IFN-α Receptor Recognition Peptide 1, associated with receptor interactions, is a peptide of IFN-α.</p>

<p>(Rac)-γ-Tocopherol (DMPBQ) is an isoform of Vitamin E that undergoes conversion to γ-Tocopherol through the action of tocopherol cyclase.</p>

<p>Guignardone L, a metabolite extracted from the endophytic fungus Guignardia mangiferae, possesses toll-like receptor 3 (TLR3) regulating activity [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>Pelgifatamab (BAY-2315497) is a prostate-specific membrane antigen (PSMA) antibody with potential anticancer activity that can be used to study prostate cancer.</p>

<p>Pepinh-MYD, a MyD88 inhibitor, incorporates both a domain sequence from MyD88 TIR and a protein transduction sequence to facilitate cell membrane penetration. This compound disrupts MyD88-mediated TLR signaling pathways, effectively inhibiting associated immune responses. Its design is particularly useful for investigating MyD88's function in viral infections.</p>

<p>2-Iminobiotin inhibits iNOS/nNOS; Ki: 21.8 μM (mouse iNOS), 37.5 μM (rat nNOS).</p>

<p>Antitumor agent-185 (compound 3) exhibits significant antitumor effects, effectively inhibiting tumor growth and extending the survival period of mice in vivo.</p>

<p>BMS986299 is a modulator of NLRP3 with an EC50 of 1.28 μM and can be used in studies about NLRP3 signaling and the treatment of associated diseases.</p>

<p>Vadastuximab (Anti-Human CD33 Recombinant Antibody) is a humanized anti-CD33 monoclonal antibody for the study of acute myeloid leukemia (AML).</p>