Inflammation/Immunology

GCN2 activator-1 (Compound 20) is a GCN2 activator. GCN2 activator-1 binds within the ATP-pocket of GCN2 and activates GCN2 in a GCN1-independent manner. GCN2 activator-1 activates Integrated Stress Response (ISR) in cells. GCN2 activator-1 inhibits PKR with an IC₅₀ of 3.75 µM. GCN2 activator-1 can be used for research of pulmonary veno-occlusive disease (PVOD).

FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC₅₀ = 3.2 nM; THP-1 cells: DC₅₀ = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC₅₀ = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis.

Ketoprofen-d₃ is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC₅₀s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively.

TLR8 antagonist-1 (Compound 10) is a selective TLR8 antagonist. TLR8 antagonist-1 can inhibit TLR8-mediated inflammation and signaling pathways, reduce the recruitment of MyD88, and inhibit the NF-κB and IRF pathways. TLR8 antagonist-1 has anti-inflammatory activity.

FITC-labeled ODN 2216 (sodium) is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. FITC-labeled ODN 2216 (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

Lepodisiran (LY3819469) is a GalNAc-conjugated small interfering RNA lipid-lowering agent. Lepodisiran targets the hepatic LPA gene and degrades apolipoprotein (a) mRNA to silence its expression, thereby effectively reducing the production of apolipoprotein (a) and serum lipoprotein (a) in a dose-dependent manner. Lepodisiran can be used in studies related to atherosclerotic cardiovascular disease.

EP4-IN-1 is a potent prostanoid EP4 receptor inhibitor. EP4-IN-1 is extracted from patent WO2023025270 (example 1), and exhibits prospect in tumor immunity and anti-inflammatory analgesia research.

PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC₅₀ of less than 1 nM. PROTAC STAT6 degrader-3 can be used for research on allergic/inflammatory diseases and cancer.

RNF5 agonist 1 (analog-1), a structural analog of RNF5 inhibitor inh-02 (HY-123967), is a potent RNF5 agonist. RNF5 agonist 1 increases the ubiquitylation status of ATG4B in F508del-CFTR-expressing CFBE41o- cells.

NLRP3 modulator 7 (Compound 17B) is a NLRP3 inflammasome modulator. NLRP3 modulator 7 inhibits LPS (HY-D1056)-induced IL-1β release in fresh human whole blood. NLRP3 modulator 7 can be used in studies related to NLRP3 inflammasome activation and innate immune signaling.

Apamistamab is a CHO-expressed human antibody that targets PTPRC/CD45. Apamistamab carries a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 146.52 kDa. The isotype control for Apamistamab can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

P2X7 receptor antagonist-2 is a potent P2X7 receptor antagonist with a pIC₅₀ value of 6.5-7.5. P2X7 receptor antagonist-2 has efficacy of combating neuroinflammation.

TD1092 is a pan-inhibitor of apoptosis protein (IAP) PROTAC degrader that targets cIAP1, cIAP2, and XIAP for degradation. TD1092 induces cell apoptosis by activating caspase. TD1092 inhibits the NF-κB signaling pathway induced by TNFα. TD1092 suppresses TNFα-induced epithelial-mesenchymal transition, cancer cell migration, and invasion. TD1092 is suitable for research on breast cancer, ovarian cancer, melanoma, and inflammation-related diseases.

Zoniporide (CP-597396) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB₂ receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity.

JNJ-1289 is a potent, selective, competitive and allosteric human spermine oxidase (hSMOX) inhibitor (IC₅₀: 50 nM). JNJ-1289 can be used in the research of polyamine catabolism, inflammation and cancers.

AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC₅₀ of 37 nM. AR-C102222 hydrochloride has antinociception and anti-inflammatory activities.

Licarin A ((+)-Licarin A), a neolignan, significantly and dose-dependently reduces TNF-α production (IC₅₀=12.6 μM) in dinitrophenyl-human serum albumin (DNP-HSA)-stimulated RBL-2H3 cells. Anti-allergic effects. Licarin A reduces TNF-α and PGD2 production, and COX-2 expression.

SMN-C2, an analog of RG-7916, is a selective modulator of SMN2 gene splicing that acts by binding SMN2 pre-mRNA, thereby increasing far upstream element binding protein 1 (FUBP1) and KH-spliced RNA binding Protein affinity regulator protein (KHSRP) to the SMN2 pre-mRNA complex. SMN-C2 can be used in spinal muscular atrophy (SMA) research.

TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC₅₀ of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC₅₀ >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis.