Immunology and Inflammation

<p>CCT374705, an orally active BCL6 inhibitor, exhibits potent antiproliferative effects in vitro and effectively inhibits tumor growth in a lymphoma xenograft</p>

11(R)-HEDE is synthesized from 11Z,14Z-eicosadienoic acid through a lipoxygenase-type reaction mediated by COX. Spectrophotometric analysis, specifically measuring the absorbance of the conjugated diene in 11(R)-HEDE, serves as an occasional method for quantifying COX activity.

<p>DNA polymerase-IN-1 exhibits antiproliferative activity against tumor cells and inhibits Taq DNA polymerase as a DNA polymerase inhibitor.</p>

<p>NLRP3-IN-9 (INF-4E) irreversibly inhibits NLRP3 ATPase, caspase-1, and prevents pyroptosis in THP-1 cells.</p>

4-Thiouracil is a photoactivatable probe designated for site-specific applications in detecting RNA structures and nucleic acid-nucleic acid contacts. Upon illumination with ultraviolet light exceeding 300 nm and in the presence of oxygen, it serves as an energy donor, facilitating the generation of singlet oxygen through triplet-triplet energy transfer. This process enables the highly reactive oxygen species to interact with 4-thiouracil, leading to the formation of uracil and uracil-6-sulfonate; the latter exhibits fluorescence around a wavelength of approximately 390 nm. Additionally, 4-Thiouracil functions as a substrate for T. gondii uracil phosphoribosyltransferase, allowing the synthesis of 4-thiouridine monophosphate for subsequent integration into RNA.

CD73-IN-4 is a potent and selective methylenephosphonic acid CD73 inhibitor

W-54011: potent non-peptide C5a receptor blocker; binds 125I-C5a (Ki=2.2nM); stops Ca2+ movement, chemotaxis, ROS in neutrophils (IC50=1.6-3.1nM).

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones.

C5aR-IN-1, a potent C5aR inhibitor, may aid in researching autoimmune and inflammatory diseases.

<p>IRAK4-IN-6 is an oral IRAK4 inhibitor with a 4 nM IC50, targeting MyD88 L265P mutant DLBCL.</p>

STING modulator-3, a 43.1 nM R232 STING inhibitor, doesn't affect IRF-3 or TNF-β in THP-1 cells.

IL-17A antagonist 3 is an IL-17A antagonist.

<p>FEN1-IN-6 (compound 9) is a potent Flap endonuclease-1 (FEN1, IC50 = 10 nM) inhibitor, crucial for DNA damage repair in mammalian cells, and additionally</p>

TMV-IN-3 is a chalcone derivative that inhibits TMV with a 120.3 μg/mL EC50, used in research on infection and cancer.

TLR7 agonist 16 (compound 16d) is a potent activator of TLR7 with an EC50 value of 18 nM.

IFN alpha-IFNAR-IN-1 HCl blocks IFN-α/IFNAR binding; IC50 2-8 μM in BM-pDCs' MVA-induced IFN-α response.

<p>Stobadine, a potent antioxidant, safeguards endoplasmic reticulum (ER) membrane fluidity against free radical-induced changes.</p>

MALT1-IN-9: potent MALT1 protease inhibitor, IC50 <500 nM in Raji cells, significant anticancer effects.

CD73-IN-11 is a potent inhibitor used to prepare medication for cancer by blocking adenosine production, which fosters tumor growth.

Argininosuccinic acid disodium, involved in the urea cycle's fourth step, is cleaved by argininosuccinate lyase (ASL) into arginine and fumarate.