Inflammation/Immunology

Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer.

RBN013209 is an orally active small molecule inhibitor of CD38 with an IC₅₀ of 0.01 to 0.1 μM for human CD38. RBN013209 prevents the conversion of extracellular NAD⁺ to ADPR or cADPR in tumor cells and PBMCs. RBN013209 can be used in the study of tumor. In addition, RBN013209 enables CAR-T cells to maintain the naive state and central memory state, and decreases the expression of cell activation markers and exhaustion-related inhibitory receptors.

Eliapixant (BAY 1817080) is a potent and selective antagonist of P2X3 receptor, with an IC₅₀ of 8 nM. Eliapixant can be used for the research of refractory chronic cough.

Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs).

Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC₅₀s of 77 nM and 6.49 μM, respectively.

SR12418 is a REV-ERB-specific synthetic ligand with IC₅₀s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.

Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation.

Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease.

Thromboxane B2 is a prostaglandin derivative that is released during anaphylaxis. Thromboxane B2 induces arterial contraction and platelet aggregation. Thromboxane B2 is a biological inactive product and circulating catabolite of thromboxane A2. Thromboxane B2 levels in peripheral venous blood and coronary sinus blood can be used as a diagnostic marker for angina. Thromboxane B2 level in serum is also associated with inhibition of COX-1 activity inhibition in platelets. Thromboxane B2 is a major product of prostaglandin endoperoxide metabolism. Thromboxane B2 produces dose-related decreases in airflow rate, tidal volume and dynamic lung compliance, whilst simultaneously increasing pulmonary airway resistance in dog model. Thromboxane B2 appears to be a naturally occurring bronchoactive metabolite in the bioconversion of arachidonic acid.

Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC₅₀s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.

Flurbiprofen-d₅ is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer.

Tellimagrandin II (Eugeniin), with oral activity, is the first intermediate of the ellagitannin series derived from ⁴C₁-glucose. It inhibits the resistance of Staphylococcus aureus by disrupting the integrity of the cell wall, leading to the loss of cytoplasmic contents. Additionally, Tellimagrandin II exhibits anti-inflammatory effects and inhibits acetylcholinesterase (AChE) activity, improving memory impairment. Tellimagrandin II holds potential for research in the fields of antibacterial, anti-inflammatory, and neurodegenerative diseases.

20-Deoxyingenol, a diterpene, is isolated from the roots of Euphorbia kansui. 20-Deoxyingenol can promote autophagy and lysosomal biogenesis by promoting the nuclear translocation of transcription factor EB (TFEB) in vitro. 20-Deoxyingenol can be used for the research of osteoarthritis (OA).

Org 274179-0 is a low-molecular-weight allosteric thyrotropin receptor (TSH Receptor) antagonist with equipotent follicle-stimulating hormone receptor antagonistic activity and selectivity for the luteinizing hormone receptor. Org 274179-0 binds to the transmembrane domain of the thyrotropin receptor, stabilizes the receptor's inactive state, and blocks agonist-induced and constitutive signaling through the adenylyl cyclase/cAMP and phospholipase C pathways. Org 274179-0 can be used for research on Graves' disease and Graves' ophthalmopathy.

A18-Iso5-2DC18 (Compound A18) is a cyclic lipidoid. A18-Iso5-2DC18 partially activates STING. A18-Iso5-2DC18 promotes mRNA protein expression and induces a strong immune response. A18-Iso5-2DC18 can be used in melanoma research.

Peripheral Myelin Protein P2 (53-78), bovine is derived from bovine peripheral myelin P2 protein amino acid residues 53-78. Peripheral Myelin Protein P2 (53-78), bovine is a T cell epitope for the induction of experimental autoimmune neuritis (EAN) in Lewis rats.

Otilimab (GSK 3196165) is an anti-granulocyte-macrophage colony-stimulating factor (GM-CSF) human monoclonal antibody. Otilimab neutralises the biological function of GM-CSF by blocking the interaction of GM-CSF with its cell surface receptor.

Ozanezumab (GSK1223249) is a humanized, Fc-inactivated monoclonal antibody that targets the nervous system protein Nogo-A. Ozanezumab promotes neurite outgrowth and axonal regeneration by neutralizing Nogo-A signaling. Ozanezumab is used for research on neurodegenerative diseases such as amyotrophic lateral sclerosis and multiple sclerosis^[1].

Hyaluronic acid sodium (MW 800kDa) is a biopolymer composed of repeating units of disaccharides with various applications. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). Hyaluronic acid sodium is synthesized at the plasma membrane. Increased hyaluronic acid sodium levels are associated with tumor cell growth, adhesion, migration, invasion and angiogenesis in digestive cancers. Hyaluronic acid sodium participates in tissue remodeling and rapid cell proliferation in some physiological processes including embryonic morphogenesis and wound-healing. Hyaluronic acid sodium activates the PI3K-Akt signaling. Hyaluronic acid sodium acts as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting proteolytic MMP-9 binding to cell surface or stimulating MMP-9 binding to cell surface. Hyaluronic acid sodium can be used as drug delivery for sodium butyrate to improve the anti-proliferative activity on breast cancer cell line. Hyaluronic acid sodium can be studied in joint diseases, wound healing and cancer.

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual-targeting PROTAC molecule. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine not only targets the ubiquitination and degradation of Smad3, but also elevates the protein level of HIF-α, thereby exerting multi-pathway anti-fibrotic and renoprotective effects. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can be used in a wide range of tumor studies including cancers with KRAS inhibitor resistance, covering pancreatic ductal adenocarcinoma, acute myeloid leukemia, and various soft tissue sarcomas (such as fibrosarcoma, liposarcoma, chondrosarcoma, etc.). (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can also be applied to research related to various solid tumors and hematological malignancies, involving multiple cancer types such as colon cancer, breast cancer, ovarian cancer, non-small cell lung cancer, glioblastoma, and melanoma.