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].
TLR7 agonist 7 (compound IIb-26) is an TLR7 agonist with an EC50 value of ~4 nM[1].
Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ[1].
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research[1].
Quercetin 3-O-neohesperidoside, a flavonoid glycoside, has anti-inflammatory activity[1].
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation[1][2][3].
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].
Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
LP117 is a novel and potent inhibitor of 5-Lipoxygenase (5-LO) product synthesis with an IC50 of 1.1 μM.
Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with an IC50 of 2.4 nM, compound 33, sourced from patent WO2018212534A1[1].
Experimental allergic encephalitogenic peptide (human) is a EAE peptide. Experimental allergic encephalitogenic peptide (human) induces encephalomyelitis in guinea pigs[1].
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G[1][2].
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].
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].
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
Lonchocarpic acid has an anti-inflammatory mechanism of lonchocarpine in LPS- or poly(I:C)-induced neuroinflammation[1].
2,4-DA-6-FP is a hapten and MR1 ligand. 2,4-DA-6-FP can used in study autoimmune diseases and cancers[1].
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].
KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent[1][2].
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].
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].
A potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays; shows no inhibitory activity against the closely related nuclear hormone receptors RORα or RORβ; attenuates expression of genes such as IL26, IL23R and CCR6 in primary human Th17 cells, attenuate the knee swelling response in an antigen-induced arthritis rat models and inhibits IL-17A cytokine production in ex vivo recall assays.
JAK3-IN-12 (compound 15k) is a highly potent JAK3 inhibitor with an IC50 value of 9.5 nM. JAK3-IN-12 can be used for researching rheumatoid arthritis[1].
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis[1].
Z-Phe-Phe-Diazomethylketone is a selective inhibitor of cathepsin L[1].