CYM50179 (compound 22n) is a potent and selective S1P4-R (Sphingosine-1-phosphate4 receptor) agonist with an EC50 of 46 nM[1].
CA-4948 is a potent, selective and orally bioavailable IRAK4 kinase inhibitor with an IC50 of < 50 nM. CA-4948 can be used for the treatment of lymphoma[1].
Sulfo-Cyanine 5 NHS Ester is a water soluble amine reactive red emitting fluorescent dye.Used for the labeling of various amine containing molecules in aqueous phase without use of any organic co-solvent. Useful for the labeling of proteins which denature in the presence of organic co-solvents, as well as for proteins with low solubility.
Lucyoside B inhibits the production of inflammatory mediators via both NF-κB and activator protein-1 pathways in activated macrophages[1].
Amcinonide inhibit NO release from activated microglia with IC50 3.38 nM. Amcinonide has affinity for the glucocorticoid receptor.IC50 value: 3.38 nM [1]Target: NO releasein vitro: Simultaneous immunofluorescent staining for T6 and Ia antigenicity within human epidermis of Amcinonide treated skin detected reduced numbers of T6+/Ia+ cells with a concomitant increase in T6+/Ia- cells. [2]in vivo: Amcinonide is an anti-inflammatory agent, elicites whitening of a few hairs in both pheomelanic and eumelanic mice. Amcinonide brings about a marked reduction in the numbers of DOPA-positive epidermal melanocytes inhabiting the tails of eumelanic or pheomelanic mice. Amcinonide exertes a deleterious influence on the structure and function of tail epidermis. [3]
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
CD80-IN-3, a potent CD80 inhibitor, inhibits CD80/CD28 interaction with an EC50 of 630 nM and a Kd of 125 nM.
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, extracted from patent WO 2019026065A2 [1].
CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
Diprovocim is a potent Toll-like receptor TLR1/TLR2 agonist that induces dose-dependent TNF production with EC50 of 110 pM in human THP-1 cells and 1.3 nM in primary mouse peritoneal macrophages; induces TNF production in bone marrow-derived dendritic cells (BMDC) with EC50 of 6.7 nM, also induces IL-6 production by mouse BMDC; induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages, activates conventional TLR1/TLR2 signaling, including MAPK and canonical NF-κB signaling; synergizes with anti-PD-L1 to eliminate melanoma in mice.
Isoflupredone belongs to the class of corticosteroids and exerts its effect by binding to glucocorticoid and mineralocorticoid receptors of animals, such as horses. Isoflupredone can be used in wide range of conditions, such as infection and inflammatory diseases[1].
KIRA-7 is a small molecule inhibitor of IRE1α kinase/Rnase with IC50 of 0.11/0.22 uM, allosterically inhibits IRE1α RNase activity; reverses bleomycin-induced fibrosis when given 2 weeks after bleomycin exposure in vivo.
Lonazolac is a non-steroidal antirheumatic agent. Anti-inflammatory effects [1].
Zaloglanstat (ISC-27864) is the inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1), and can be used to study asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases, etc[1].
Monomethyl fumarate-d5 is deuterium labeled Monomethyl fumarate. Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease[1][2][3].
GB-88 is a selective, orally PAR2 antagonist, inhibits PAR2 activates Ca(2+) release with an IC 50 of 2 µM[1].
Icosabutate, a structurally engineered and orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis[1]. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia [2].
A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively; >15-fold selectivity for TRPV4 over TRPV1, TRPV3 and TRPM8, and a panel of 54 other common biological targets.
Benzothiazole is a natural occurring heterocyclic nuclei. Benzothiazole nucleus possesses a number of biological activities such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, antiviral, antileishmanial, and antiviral[1].
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1)[1].
3,4-O-Isopropylidene-shikimicn acid is a natural product that can be isolated from the whole plants of Hypericum wightianum. 3,4-O-Isopropylidene-shikimic acid has anti-inflammatory effect and antioxidant activities[1][2].
MRGPRX4 agonist-1 (compound 30d) is a selective agonist of MRGPRX4 with EC50s of 11.2 nM and 30.0 nM in Ca2+ and β-arrestin experiments, respectively[1].
ACAT-IN-9 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 207. ACAT-IN-9 inhibits NF-κB mediated transcription[1].
Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE)[1][2].
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation[1].
Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia[1][2][3][4].
Thrombospondin-1 (1016-1023) (human, bovine, mouse), is the C-terminal end of the native sequence of Thrombospondin-1 (TSP-1), is a CD47 agonist peptide[1].
Z-Phe-Phe-Diazomethylketone is a selective inhibitor of cathepsin L[1].
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice[1].