Eckol is a potent hMAO-A (Mixed) and hMAO-B (non-competitive) inhibitor with IC50s of 7.20 and 83.44 μM, respectively. Eckol shows stimulatory effects in maize and can be used as a plant biostimulant. Eckol also shows antiallergic and antiviral effects[1][2][3][4].
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties[1][2][3][4].
BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1)[1].
Xanthone is isolated from Mangosteen and is known to control cell division and growth, apoptosis, inflammation, and metastasis in different stages of carcinogenesis. Xanthone has anti-oxidant, anti-tumor, anti-allergic, anti-inflammatory, anti-bacterial, anti-fungal, and anti-viral activities[1].
Loureirin C, isolated from "Dragon’s blood", which is a deep red resin obtained from a variety of plant sources. The resin extracted from stems of Dracaena cochinchinensis is one such source of “dragon’s blood”, has a reputation for facilitating blood circulation and dispersing blood stasis. The resin has anti-bacterial, anti-spasmodic, anti-inflammatory, analgesic, anti-diabetic, and anti-tumor activities[1].
(E/Z)-HA155 is a potent autotaxin (ATX) type I inhibitor. (E/Z)-HA155 can be used for researching cancer, fibrotic diseases, inflammation, pain and angiogenesis[1].
Dihydrocatalpol can be isolated from Rehmannia glutinosa. Dihydrocatalpol can be used for research on Asthma, chronic obstructive pneumonia, allergic rhinitis[1].
Coronalolic acid, extract from the apical bud of Gardenia sootepenesis Hutch, inhibits TNF-α-induced NF-κB activity and NO production[1].
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis[1][2][3].
VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM; is more selective for fungal CYP51 than related human CYP enzymes such as CYP3A4; exhibits excellent potency against yeast, dermatophyte, and mold fungal pathogens.
Mepolizumab (SB 240563) is a humanized monoclonal antibody that binds to and neutralizes interleukin-5 (IL-5), the major cytokine involved in eosinophil proliferation, activation, and survival. Mepolizumab can be used for the research of eosinophilic granulomatosis with polyangiitis (EGPA) and severe eosinophilic asthma[1][2].
Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Interphotoreceptor Retinoid Binding Protein Fragment (IRBP), a 20-residue peptide and a major pathogenic epitope, is present in the first homologous repeat of the interphotoreceptor retinoid binding protein peptide (IRBP 161–180), which can induce posterior uveitis (EAU)[1].
Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression[1].
GSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation[1][2].
GPR183 antagonist SAE-14 is a potent, selective GPR183 antagonist with IC50 of 28.5 nM, inhibits GPR183-dependent 7α,25-dihydroxycholesterol-induced calcium signaling in HL-60 cells.GPR183 antagonist SAE-14 inhibits calcium mobilization induced by 7α,25-OHC (EC80 209 nM).GPR183 antagonist SAE-14 reversed CCI-induced mechanical allodynia in a time-dependent manner when administered in vivo to mice.7α,25-dihydroxycholesterol induced allodynia in mice, SAE-14 blocked the effects of 7α,25-OHC in a dose-dependent manner.
1-Pentadecanol-d31 is the deuterium labeled 1-Pentadecanol[1]. 1-Pentadecanol is a naturally occurring antiacne agent[2].
NF-κB-IN-13 (compound 12) can significantly inhibit LPS-induced NF-κB activation and NO production in RAW264.7 macrophages. NF-κB-IN-13 has anti-inflammatory effects[1].
Lipofundin S is an emulsion containing soy bean oil, soy phosphatides & glycerol.
Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models[1].
Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.
3,4,5-Tricaffeoylquinic acid is isolated from barks of Ilex rotunda Thunb, used in the research of the pro-inflammatory mediator-induced skin disease[1].
SEMBL is a potent NF-κB inhibitor that inhibits DNA binding of NF-κB component p65; inhibits LPS-induced NF-κB activation, iNOS expression, and inflammatory cytokine secretions; also inhibits NF-κB and cellular invasion in ovarian carcinoma ES-2 cells; enhances stability in aqueous solution compared with (-)-DHMEQ.
Protirelin is a highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions.
GNE-4997 is a potent and selective ITK/TSK inhibitor.
Zastaprazan is a proton pump inhibitor (WO2018008929). Zastaprazan can be used for the research of gastrointestinal inflammatory diseases or gastric acid-related diseases[1].
Trimetazidine-N-oxide is the major active metabolite of Trimetazidine. Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM. Trimetazidine is an effective antianginal agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties.
RIPK1-IN-16 is an orally active and potent inhibitor of RIPK1. RIPK1-IN-16 inhibits excessive inflammation by blocking RIPK1-mediated necroptosis in vivo. RIPK1-IN-16 protects mouse from TNF-induced systemic inflammatory response syndrome and sepsis[1].
Purotoxin 1 is a P2X3 receptor inhibitor. Purotoxin 1 shows antinociceptive properties in animal models of inflammatory pain. Purotoxin 1 can be isolated from the venom of the wolf spider Geolycosa sp[1].