Pathogens Infection

FXIIa-IN-6 is a potent, selective, and irreversible covalent inhibitor of Factor XIIa (FXIIa) with an IC₅₀ of 2 nM. FXIIa-IN-6 exhibits ≥2,500-fold selectivity over related serine proteases. FXIIa-IN-6 exhibits favorable anticoagulant and anti-inflammatory activities and can be used in sepsis research.

OI-3 is a monoclonal antibody targeting CD146 (MCAM). OI-3 specifically binds to CD146 on the surface of human mesothelioma cells and undergoes endocytosis; both chimeric (chOI-3) and murine (mOI-3) variants possess this activity. When conjugated with ²¹²Pb to form ²¹²Pb-TCMC-OI-3, OI-3 acts as a cytotoxic agent that delivers α-emitting radionuclides to induce targeted cytotoxicity. OI-3 can be used in research related to malignant peritoneal mesothelioma.

15-PGDH-IN-5 is a sulfoxide-based inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH). 15-PGDH-IN-5 exhibits great water solubility, metabolic stability, and in vivo exposure levels. 15-PGDH-IN-5 blocks the 15-PGDH-mediated irreversible oxidative degradation of PGE2 and increases the effective concentration of endogenous PGE2 in tissues, thereby exerting anti-inflammatory effects and promoting tissue repair and regeneration. 15-PGDH-IN-5 is suitable for research into tissue injury and fibrosis-related diseases, such as inflammatory bowel disease and idiopathic pulmonary fibrosis.

TSI-13-48 (HY-182409) is a TLR inhibitor with IC₅₀ values of 3.02, 22.3, 26.5, and 26.6 μM against TLR9, TLR7, TLR2, and TLR4, respectively. TSI-13-48 can be used in research related to systemic lupus erythematosus, polymicrobial sepsis, and cerebral malaria.

DT-5461 is an IL-1 and TNF-α antagonist. DT-5461 competitively binds lipid A-binding sites on macrophage receptors, blocks LPS (HY-D1056)-initiated signaling, inhibits LPS-induced cytokine release, prevents LPS-induced serum cytokine production in mice, and protects against LPS-induced lethal endotoxemia. DT-5461 can be used for the research of lethal endotoxemia, medullary tubular mammary carcinoma, poorly differentiated colon adenocarcinoma, squamous-cell lung carcinoma, and gelatinous gastric adenocarcinoma.

ODZ10117 is a STAT3 and NLRP3 inhibitor with a human STAT3 SH2 domain IC₅₀ of 7.5 μM. ODZ10117 binds to the STAT3 SH2 domain, suppressing tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity. ODZ10117 binds to NLRP3, impairs NEK7 interaction, prevents inflammasome formation, and inhibits caspase-1 and IL-1β cleavage.ODZ10117 reduces MSU (HY-B2130A)-induced IL-1β release, lowers LPS (HY-D1056)-induced sepsis mortality, and exhibits anti-inflammatory effects. ODZ10117 induces apoptosis, suppresses breast cancer cell migration and invasion, reduces tumor growth and lung metastasis, and extends survival in breast cancer models. ODZ10117 can be used for the research of Monosodium urate (HY-B2130A)-induced peritonitis, LPS-induced sepsis, breast cancer, glioblastoma, and Alzheimer's disease.

CSLP43 is a selective RIPK2 and XIAP inhibitor with an IC₅₀ of 19.9 nM against human RIPK2. CSLP43 binds to the ATP-binding pocket of RIPK2 and disrupts the interaction between RIPK2 and the BIR2 domain of XIAP or cIAP1. CSLP43 inhibits RIPK2 ubiquitination, NOD1-dependent inflammatory signaling pathways, NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation associated with NOD agonists. CSLP43 is selective for the NOD1/NOD2 signaling pathway and does not inhibit the kinase activity of RIPK1 or RIPK3. CSLP43 is applicable to research related to Crohn's disease, Blau syndrome, early-onset sarcoidosis and early-onset inflammatory bowel disease.

SX-576 is a CXCR1 and CXCR2 antagonist with IC₅₀ values of 31 nM and 21 nM, respectively. SX-576 inhibits neutrophil infiltration in a rat model of pulmonary inflammation. SX-576 can be used in studies related to pulmonary inflammation.

S-Petasin is a phosphodiesterase (PDE) inhibitor with IC₅₀ values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis.

O-Demethylrotenone is a rotenone (HY-B1756) derivative and a photodegradation product of rotenone that induces acute intraperitoneal toxicity. The acute intraperitoneal LD₅₀ of O-Demethylrotenone in Mus musculus is 8.0 mg/kg.

Lb54 is a caspase-3 and caspase-7 activator with an EC₅₀ of 660.9 nM for human procaspase-3. Lb54 activates caspase-3/7, which cleaves Gasdermin D (GSDMD) at aspartic acid residue 87 to generate a p10 fragment, preventing formation of the pore-forming p30 fragment of GSDMD. Lb54 suppresses GSDMD-mediated pyroptosis through caspase-3/7 activation, thereby attenuating inflammatory responses and conferring protection against sepsis. Lb54 alleviates acute lung injury, and inhibited systemic inflammation by restraining the maturation of monocyte-derived dendritic cells. Lb54 can be used for the research of sepsis.

Antitubercular agent-56, a Questiomycin A (HY-N8439) derivative, is a potent and orally active antitubercular agent. Antitubercular agent-56 disrupts mycobacterial envelope integrity by inhibiting FabD (K_d = 9.39 μM; IC₅₀ = 49.60 μM). Antitubercular agent-56 exhibits good intracellular antimycobacterial activity against Mycobacterium tuberculosis (MTB) and drug-resistant MTB both in vitro and in vivo. Antitubercular agent-56 can be used for research on tuberculosis (TB).

Ensifentrine (RPL-554) tosylate is an inhaled dual inhibitor of PDE3 and PDE4 with IC₅₀s of 0.4 nM and 1479 nM, respectively. Ensifentrine tosylate blocks PDE3 and PDE4 enzymes, thereby increasing the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, dilating the bronchi, and inhibiting the activation and migration of inflammatory cells. Ensifentrine tosylate can be used in the research of chronic obstructive pulmonary disease (COPD).

HDAC3 degrader-1 (Compound Z8) is a selective HDAC3 degrader with a DC₅₀ of 2.42 μM. HDAC3 degrader-1 has almost no effect on HDAC1, HDAC2, and HDAC6. HDAC3 degrader-1 inhibits the activation of the NLRP3 inflammasome and reduces the secretion of IL-1β and caspase-1. HDAC3 degrader-1 shows significant efficacy in septic shock and colitis models. HDAC3 degrader-1 can be used in anti-inflammatory research.

R 58639 is a histamine H1 receptor antagonist. R 58639 can be used for the study of gastric ulcers.

BVL3572S, a hydroxamic acid derivative, exhibits potent bactericidal activity against Mycobacterium tuberculosis (Mtb) with a MIC₉₀ of 1.7 µM. BVL3572S inhibits pyridoxal phosphate (PLP)-dependent aminotransferases HisC and AlaA to kill Mtb. BVL3572S can be used for tuberculosis (TB) research.

Famotidine-¹³C₃ (MK-208-¹³C₃) is the ¹³C₃-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

Famotidine-d₄ (MK-208-d₄) is the deuterated-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

Apidaecin IA is a basic peptide. Apidaecin IA inhibits the enzymatic activity of DnaK. Apidaecin IA induces bacterial cell death. Apidaecin IA can be used in research related to peritonitis and bacterial infections.

DL-Cycloserine-¹⁵N,d₃ is the deuterium labeled DL-Cycloserine (HY-W008440). DL-Cycloserine is an orally active aminotransferase inhibitor. DL-Cycloserine exhibits completely opposite effects on the activity of monoamine oxidase in different tissues. DL-Cycloserine can be used for the research of pulmonary tuberculosis, psychosomatic diseases, and depressive states.