RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis[1][2].
Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis[1][2].
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury[1][2][3].
Magnesium silicate (Activated magnesium silicate) is a compound of magnesium oxide (MgO) and silicon dioxide (SiO2). Magnesium silicate is used in antiacid and antiulcer preparation, and as a deodorizer, decolorizer and antifungal[1].
COX/5-LOX-IN-1 (compound 6b) is a potent and dual inhibitor of COX/5-LOX with IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively. COX/5-LOX-IN-1 has the potential for the research of inflammation diseases[1].
Antitumor agent-56 (Compound 33) is a triptolide derivative with antitumor, anti-inflammatory and NO release activities. Antitumor agent-56 significantly inhibits the growth of melanoma. Antitumor agent-56 is orally active[1].
SARS-CoV-2-IN-66 (1), a vitaminK derivative, is a SARS-CoV-2 inhibitor, with an EC50 of 70.8 μM in VeroE6/TMPRSS2 cells[1].
NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells[1].
Chlorthenoxazine is a nonsteroidal anti-inflammatory drug.
MSA-2 is an orally available non-nucleotide STING agonist, with EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1].
Bulbocapnine hydrochloride, an aporphine alkaloid, is a dopamine receptor inhibitor. Bulbocapnine hydrochloride inhibits dopamine synthesis. Bulbocapnine hydrochloride also has neuroleptic-like, anticonvulsant and antinociceptive effects[1][2][3].
Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure[1].
3-pyridine toxoflavin is an impurity of toxoflavin.
Tripelennamine, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine lessens the allergic response of the organism caused by histamine. Tripelennamine can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions[1][2][3].
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia[1].
Enterobactin is a bacterial siderophore that promotes iron absorption and can be used to study inflammation. Enterobactin also disrupts macrophage (MΦs) iron homeostasis and M1/M2 polarization to protect intracellular bacteria from host antimicrobial effects[1].
Homocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects[1].Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation[2].
WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).EC50 value: 28 nM [1]Target: β cell proliferation agonistProtocol(Only for Reference) [1]In vivo efficacy studies in RIP-DTA mice:RIP-DTA mice were purchased from Jackson Laboratories and all aspects of their treatment were outlined in a protocol approved by an internal animal care and use committee (IACUC). Mice were housed as 3-5 mice per cage and fed standard chow and water. During disease induction, doxycycline was added to the drinking water at a concentration of 2 mg/mL. Animals were injected intraperitoneally with saline-formulated WS6 at 5 mg/kg once every other day (for efficacy study). Blood glucose was monitored every third day. Mice were sacrificed at the end of week 1 and pancreas was fixed in formalin, sectioned, and stained for Ki67 and insulin. At the end of week 6, wet pancreas weight was recorded, and fixed pancreata were sectioned and stained for insulin; total insulin area and wet weight were used to calculate beta cell mass. For pharmacokinetic studies, WS6 was formulated at 50 mg/kg and given as single intraperitoneal dose, followed by serum collection and analysis of compound concentration in serum to determine CMAX and half-life (T1/2).
Homobutein a natural chalcones (can be found in many medicinal plants, fruits, vegetables, spices and nuts), is a potent HDACs/NF-κB dual inhibitor with IC50s of 190 and 38 μM, respectively. Homobutein also a chelator of iron (II and III) cations, shows various activities, including anticancer, anti-inflammatory, antiparasite and antioxidation[1][2][3][4].
Lewis X trisaccharide (Lewis X, Lex) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis[1][2][3].
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl－ secretion in T84 colonic cells[1]. DCEBIO stimulates Cl－ secretion via the activation of hIK1 K＋ channels and the activation of an apical membrane Cl－ conductance[2].
Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT)[1].
Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models[1][2].
LP117 is a novel and potent inhibitor of 5-Lipoxygenase (5-LO) product synthesis with an IC50 of 1.1 μM.
Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties[1][2].
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile[1].
Rabdosiin is a tetramer of caffeic acid isolated from the stem of Rabdosia japonica Hara. Rabdosiin possess anti-allergic activity, anti-HIV activity and inhibition on DNA topoisomerase[1].
cis-5-Dodecenoic acid is an endogenous metabolite with inhibitory activities against COX-I and COX-II[1].
MC-D-Val-Cit-PAB-PNP is a drug-linker-ligand conjugates. MC-D-Val-Cit-PAB-PNP can be used for researching cancer, autoimmune diseases and infectious diseases[1].