Immunology and Inflammation

<p>MALT1-IN-5 is a potent inhibitor of the MALT1 protease and can be used in cancer research.</p>

<p>COX-2/PI3K-IN-2 (5f): anti-inflammatory &amp; anti-cancer, selectively inhibits COX-2 (Ki=3.02nM), potently blocks PI3K (IC50=2.78nM).</p>

<p>Anti-inflammatory agent 102 (Compound 11a) is an orally effective anti-inflammatory compound. It exerts its effects by inhibiting the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. This agent displays significant anti-inflammatory activity by suppressing the release of NO, ROS, and inflammatory cytokines such as IL-6, TNF-α, and IL-1β. Anti-inflammatory agent 102 is applicable in research concerning inflammatory diseases, including ulcerative colitis (UC).</p>

<p>CD73-IN-13, a potent CD73 inhibitor, may be developed for tumor-related disease treatment.</p>

<p>IRAK4-IN-14 is a selective, potent, orally active IRAK4 inhibitor (IC50: 0.003 μM) with favorable PK parameters in rats and mice. effect.</p>

<p>COX-2/15-LOX-IN-5 (Compound 4f) functions as a dual inhibitor of COX-2 and 15-LOX, demonstrating both anti-inflammatory and antioxidant properties [1]. This compound effectively reduces NF-κB activation in RAW 264.7 macrophages that is induced by lipopolysaccharide.</p>

<p>ODN 21158 is a potent, non-cytotoxic inhibitor of G-modified TLR3 and TLR9. ODN 21158 dose-dependently inhibits IFN-α secretion.</p>

<p>MAO-B-IN-7 inhibits MAO-B/AChE, crossing the blood-brain barrier; IC50: 41/87 nM (h/eel AChE), 0.3 μM (MAO-B). Reduces oxidative stress and neuroinflammation.</p>

<p>CB-1158 is a potent and orally bioavailable inhibitor of arginase (IC50s: 86 and 296 nM for recombinant human arginase 1 and 2).</p>

<p>GNE-2256, also known as molecule 19, is an orally active compound that inhibits Interleukin 1 receptor-associated kinase 4 (IRAK4) with a K i of 1.4 nM and has</p>

<p>TLR7/8 agonist 7 activates immune cells, useful in ISAC synthesis and immunity research.</p>

<p>COX-2-IN-7: potent, orally active COX-2 inhibitor with higher selectivity than Celecoxib, IC50 6.585 uM, anti-inflammatory, low ulcer risk.</p>

<p>TLR4/JNK/NF-κB-IN-1 (Racemic-11k) is an inhibitor of TLR4, JNK, and NF-κB. It suppresses NO production in LPS-stimulated RAW264.7 cells with an IC50 of 23.2 µM. By inhibiting TLR4 expression and reducing JNK phosphorylation, TLR4/JNK/NF-κB-IN-1 prevents NF-κB activation. This leads to a decrease in the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and the production of inflammatory mediators such as NO, PGE2, and TNF-α, thereby exhibiting anti-inflammatory activity. TLR4/JNK/NF-κB-IN-1 holds potential in the study of inflammatory diseases, including rheumatoid arthritis and various other inflammatory conditions.</p>

<p>Compound O15, an Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM; it inhibits Keap1-Nrf2 binding and Nrf2 ubiquitination.</p>

<p>meso-Zeaxanthin accumulates in the central retina and, together with lutein and zeaxanthin, forms the macular pigment, which functions as a light filter. meso-Zeaxanthin can quench reactive oxygen species (ROS), thereby exhibiting antioxidant properties.</p>

<p>(S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1. This interaction leads to the ubiquitination and subsequent proteasomal degradation of MALT1. By disrupting the CBM complex, (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway and shows potential in inducing apoptosis in ABC-DLBCL cells. It holds promise for research into MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL).</p>

<p>IL-17 modulator 5 is a IL-17 inhibitor, with an IC 50 of 1 nM .</p>

<p>IRAK4-IN-11 (compound 6) is a potent inhibitor of IRAK4 with an IC 50 of 0.008 μM. IRAK4-IN-11 exhibits cell pIRAK4 potencies with an IC 50 of 0.19 μM [1].</p>

<p>TLR7/8 antagonist 2: potent, orally active, IC50: 4.9 nM (TLR7), 0.6 nM (TLR8); potential for lupus therapy research.</p>

<p>XO/COX/LOX-IN-1 targets XO/COX/LOX, used in research of inflammation, cancer, and metabolic disorders.</p>