Ebselen is a small-molecule capsid Inhibitor of HIV-1 replication.Target:Ebselen is an organoselenium compound, as an inhibitor of HIV-1 capsid CTD dimerization. Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process. [1] Ebselen is a non-toxic seleno-organic drug with anti-inflammatory and antioxidant properties. Ebselen is an inhibitor of inositol monophosphatase (IMPase). Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. [2]
Tormentic acid, a triterpene isolated from Rosa rugosa, exerts anti-inflammatory, antihyperlipidemic, and anti-atherogenic properties[1][2].
ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.
JAK-IN-28 (Compound 111) is a JAK inhibitor. JAK-IN-28 can be used for research of cancer or inflammatory diseases[1].
4-Thiouridine 5′-triphosphate (4-Thio-UTP) tetralithium is a potent P2Y2 and P2Y4 receptor agonist, with EC50s of 35 and 350 nM for hP2Y2 and hP2Y4, respectively. 4-Thiouridine 5′-triphosphate tetralithium can be used in the study of crosslinking experiments, labeling of transcriptional complex[1][2].
Tabalumab (LY2127399) is a humanised anti-BAFF (B-cell activating factor) monoclonal antibody (IgG4 type) with neutralising activity against membrane bound and soluble BAFF. Tabalumab can be used in studies of autoimmune diseases such as rheumatoid arthritis, renal failure and systemic lupus erythematosus[1].
Ambutonium bromide is an acetylcholine antagonist.
A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively; inhibits CXCL1-induced Ca(2+) flux in human PMNs but has no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF; antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation in recombinant HEK293 cells expressed CXCR2; significantly inhibits inflammation in an in vivo murine model (0.2 mg/kg iv).
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine mesylate is used for the study of rheumatoid arthritis (RA)[3].
Vitisin A has antioxidative, anticancer, antiapoptotic, neuroprotective and anti-inflammatory effects. Vitisin A inhibits LPS-induced NO and iNOS production via down-regulation of ERK1/2 and p38 and the NF-κB signal pathway. Vitisin A also inhibits adipocyte differentiation. Vitisin A is a resveratrol tetramer that can be isolated from Vitis vinifera roots[1][2][3].
Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT)[1].
Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1.
Emapalumab (NI-0501) is a humanized monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH)[1].
COX-2/5-LOX-IN-2 (5b) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-2 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-2 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 5.40, 0.01 and 1.78 μM, respectively[1].
NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.IC50 value: 9 nM [1]Target: KCa3.1 channel inhibitorin vitro: NS6180 inhibited cloned human KCa3.1 channels (IC50 = 9 nM) via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15–20 nM). NS6180 suppressed rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-γ production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production [1].in vivo: DNBS challenged rats were treated with two doses (3 and 10 mg·kg-1 b.i.d.) of NS6180 for 7 days in direct comparison with the IBD drug sulfasalazine (300 mg·kg-1 q.d.). Both doses of NS6180 significantly improved weight gain and decreased inflammation induced swelling of the colon as determined by relative colon weight [1].
Leniolisib (CDZ173) phosphate is a potent and selective PI3Kδ inhibitor. Leniolisib phosphate has the potential for immunodeficiency disorders treatment.
Glucosamine-13C hydrochloride is the 13C labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a
Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. Piriprost potassium inhibits the release of both leukotriene and histamine with an IC50 of 0.11 μM from isolated porcine lung cells. Piriprost potassium increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells[1][2].
ATB-346 is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity.IC50 value:Target: COX-2 ATB-346 suppressed gastric prostaglandin E(2) synthesis as effectively as naproxen, but produced negligible damage in the stomach and intestine, Unlike naproxen and celecoxib, ATB-346 accelerated healing of pre-existing gastric ulcers. In a mouse airpouch model, ATB-346 suppressed cyclooxygenase-2 activity and inhibited leukocyte infiltration more effectively than naproxen. ATB-346 was as effective as naproxen in adjuvant-induced arthritis in rats, with a more rapid onset of activity. Unlike naproxen, ATB-346 did not elevate blood pressure in hypertensive rats [1]. Treatement with ATB-346 exhibited a significantly more rapid and sustained recovery of motor function, achieving greater than double the increase in locomotion score of the naproxen group by the 10th day of treatment. ATB-346 also significantly reduced the severity of inflammation (proinflammatory cytokines, apoptosis of neural tissue, and nitrosative stress) that characterized the secondary effects of SCI [2].
1,6-Dihydro-4,7-epoxy-1-methoxy-3,4-methylenedioxy-6-oxo-3,8-lignan, a lignan derivative from the ethyl acetate soluble fraction of twigs of Magnolia denudate (Magnoliaceae), exhibits anti-platelet-activating factor (PAF) activity. PAF is a potent lipid mediator in inflammation and asthma[1].
Betulinic acid derivative-1 exhibits distinguished activities on inhibiting osteoclast (OC) differentiation with an IC50 value of 1.86 μM.
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.IC50 value:Target: GATA-specific inhibitorin vitro: K-7174 inhibited the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either tumor necrosis factor alpha or interleukin-1beta, without affecting the induction of intercellular adhesion molecule-1 or E-selectin. K-7174 had no effect on the stability of VCAM-1 mRNA.K-7174 did not influence the binding to any of the following binding motifs: octamer binding protein, AP-1, SP-1, ets, NFkappaB, or interferon regulatory factor [1]. Addition of 10 microM K-7174 rescued these inhibitions of Epo protein production and promoter activity induced by IL-1beta, TNF-alpha, or L-NMMA, respectively [2]. K-7174 had the potential to induce endoplasmic reticulum (ER) stress evidenced by induction of GRP78 and CHOP.Other inducers of ER stress completely reproduced the effects of K-7174 including suppression of lipid accumulation, blockade of induction of adiponection and PPARgamma and maintenance of MCP-1 expression [3].in vivo: K-7174, one of proteasome inhibitory homopiperazine derivatives, exhibits a therapeutic effect, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. Moreover, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [4].
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease[1].
Sequifenadine is a H1-antihistamine. Sequifenadine has the potential for the research of inflammatory eye disease with allergic symptoms[1][2].
ARN16186;ARN 16186;ARN-16186
FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration[1].
Velutin is an aglycone extracted from Korean Mistletoe, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway[1][2].
(S)-Veliflapon ((S)-BAY X 1005; (S)-DG-031) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood[1][2][3].
Floctafenine, a nonsteroidal anti-inflammatory agent (NSAID), acts as an effective analgesic agent[1][2]. Floctafenine is an inhibitor of COX-1 and COX-2 activities in vitro,showing a slightly higher potency towards COX-I. Floctafenine is used for the research of short term pain treatment[3].
Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models[1].