1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties[1]. 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells[2].
H4R antagonist 3 (Example 18) is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. H4R antagonist 3 can be used for the research of prevention of inflammatory, autoimmune, allergic, and ocular diseases[1].
DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.
IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).IC50 value:Target: IFN alpha-IFNAR interaction inhibitorIFN alpha-IFNAR-IN-1 specifically inhibits MVA-induced IFN-α responses by BM-pDCs. IFN alpha-IFNAR-IN-1 inhibited the IFN-α responses that were elicited after treatment with CpG2216, stimulation with poly(I:C), and infection with VSV-M2, whereas the total IL-12 production was notably less affected under those conditions. IFN alpha-IFNAR-IN-1 exerts immunosuppressive activity by the direct interaction with IFN-α [1].
LP99 is the first potent and selective BRD7/9 bromodomain inhibitor with Kd of 99 nM for BRD9; inhibits IL‐6 secretion from THP‐1 cells in a dose‐dependent manner; decreases BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose‐dependent manner, with cellular IC50 values in the low micromolar range for both histones.
BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.IC50 value: 7.5 nM (Ki) [1]Target: Sykin vitro: BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606 [1]. We identified BAY61-3606 as an inhibitor of proliferation in colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS. In addition to its anti-proliferative effects in mutant cells, BAY61-3606 exhibited a distinct biological property in wild-type cells in that it conferred sensitivity to inhibition of RAF. In this context, BAY61-3606 acted by inhibiting MAP4K2 (GCK), which normally activates NFκβ signaling in wild-type cells in response to inhibition of RAF [2].in vivo: Oral administration of BAY 61-3606 to rats significantly suppressed antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuated antigen-induced airway inflammation in rats [1].
Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains[1].
Piperidinylaminomethyl Trifluoromethyl Cyclic Ether Compound 1 has the potential function in central nervous system disorders, respiratory, inflammatory diseases and gastrointestinal disorders.
SB-226552 is an aryloxypropanolamine selective beta3AR agonist.
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro[1][2][3][4].
(R)-Reticuline is an isomer of Reticuline (HY-N1356). Reticuline displays anti-inflammatory and cardiovascular effects through JAK2/STAT3 and NF-κB signaling pathways. Salutaridine is a key intermediate in morphine biosynthesis. Salutaridine can be converted from (R)-Reticuline in the poppy plant. The conversion system relies on membrane-bound cytochrome P-450 enzymes and also requires reducing cofactors NADPH, molecular oxygen, etc[1][2].
N-Acetyldopamine dimer-2 (compound 2) is a N-acetyldopamine dimer that can be isolated from the yellow powder form Periostracum Cicadae with antioxidant and anti-inflammatory activities. N-Acetyldopamine dimer-2 inhibits oxidized low-density lipoprotein (LDL) oxidation, ROS generation, NO production, and NF-κB activity[1].
Influenza HA (110-119) is the 110-119 fragment of influenza virus hemagglutinin that can stimulate Treg cells proliferation[1][2].
Cromoglicic acid-d5 is the deuterium labeled Cromolyn[1]. Cromolyn is a mast cell stabilizer. Cromolyn has the potential for the research of bronchial asthma, allergic rhinitis, and certain allergic eye conditions such as vernal conjunctivitis, keratitis, and keratoconjunctivitis[2].
Cenegermin is a recombinant human nerve growth factor (rhNGF). Cenegermin can be used in the research of neurotrophic keratitis[1].
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity[1]. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function[2].
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations[1].
Liensinine Perchlorate is a constituent of Nelumbo nucifera Gaertn, with ani-hypertension and anti-cancer activities. Liensinine Perchlorate induces colorectal cancer (CRC) cell apoptosis[1].
RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
Opinercept is a tumor necrosis factor-alpha (TNF-alpha) inhibitor. Opinercept can be used for the research of rheumatoid arthritis (RA)[1].
Trepibutone (AA 149) increases secretion of bile and pancreatic juice, and accelerates flaccidity of the smooth muscle in the gastrointestinal tract. Trepibutone can be used for the research of cholecystitis and functional gastrointestinal disorders[1][2].
Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α，5-HT1β and 5-HT2，respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].
LH 1 is an immunostimulant used in antitumor treatment.
Brompheniramine maleate is a histamine H1 receptors antagonist.Target: Histamine H1 ReceptorBrompheniramine maleate, is an antihistamine drug of the propylamine (alkylamine) class. It is readily available over the counter and is indicated for the treatment of the symptoms of the common cold and allergic rhinitis. It is a first-generation antihistamine. Brompheniramine has antidepressant properties, inhibiting reuptake of the neurotransmitter serotonin. Based on this knowledge, Arvid Carlsson and his colleagues, working at the Swedish company Astra AB, were able to derive the first marketed selective serotonin reuptake inhibitor, zimelidine, from brompheniramine. Brompheniramine had a long half-life and large volume of distribution in normal adults. It also had a prolonged antihistaminic effect in the skin as evidenced by suppression of the wheal and flare response to histamine and by suppression of pruritus [1, 2].
Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3].
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also a selective ligand of the GPR35 receptor.
Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively[1][2].
Kadsurin, a natural compound from the stems of Kadsura heteroclita (Schizandraceae), results in significant decreases of CCL4- induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice[1].
L-745337 is a selective cyclooxygenase-2 (COX2) inhibitor, with an IC50 of 2.3 nM, and shows anti-inflammatory activity.