PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50 of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
Bryonolic acid is an active triterpenoid compound with immunomodulatory, anti-inflammatory, antioxidant and anticancer activities[1][2][3].
3-Deoxysappanchalcone is a naturally-occurring chalcone compound isolated from Caesalpinia sappan L. (Leguminosae), which possesses anti-allergic, antiviral, anti-inflammatory and antioxidant activities. 3-Deoxysappanchalcone exerts anti-inflammatory activity via induce heme oxygenase-1 (HO-1) expression by activating the AKT/mTOR pathway in murine macrophages. 3-Deoxysappanchalcone also exhibits anti-influenza virus activity (H3N2, IC50 = 1.06 μM)[1][2].
Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and active human vitiligo and exhibits good potential for vitiligo research[1].
MMP-9-IN-6 (Compound 3g) is a MMP-9 inhibitor with IC50 value of 50 μM, which has good anti-ulcer effect[1].
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases[1].
Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive drug.
Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker. Seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm[2]. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat[1].Xanthopterin hydrate inhibits RNA synthesis[4].
Coblopasvir (KW136, KW-136) is a novel HCV NS5A inhibitor under development for treatment of HCV infection. HCV Infection Phase 3 Clinical
Acetylcorynoline is the major alkaloid component derived from Corydalis bungeana, and has anti-inflammatory properties[1].
Ro26-4550 is a low micromolar antagonist of IL-2/IL-2Rα binding with an IC50 value of 3 μM[1].
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase[1].
Ginsenoside F4 (GF4), ginseng saponinis, isolated from notoginseng or red ginseng. Ginsenoside F4 (GF4) has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis[1].Ginsenoside F4 (GF4) inhibits matrix metalloproteinase 13 (MMP 13) expression in IL-1β-treated chondrocytes and blocks cartilage breakdown in rabbit cartilage tissue culture, shows therapeutic potential for preventing cartilage collagen matrix breakdown in diseased tissues[2].
UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
Cetirizine methyl ester is an impurity of Cetirizine (HY-17042). Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1].
3-O-(2'E,4'Z-Decadienoyl)ingenol is a natural diterpene that exhibits significant anticomplement activity with an IC50 of 89.5 μM[1].
CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.
Andolast is an anti-allergic agent for the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD). Andolast inhibits dose dependently guinea-pig lung cAMP-phosphodiesterase with an IC50 of 50 mM.
Edpetiline is a principal alkaloid from P. eduardi. Edpetiline has significant antiinflammatory effects[1].
Robinin is present in flavonoid fraction of Vigna unguiculata leaf. Robinin inhibits upregulated expression of TLR2 and TLR4. Robinin ameliorates oxidized low density lipoprotein (Ox-LDL) induced inflammatory insult through TLR4/NF-κB pathway[1].
L 691816 is a potent, selective and orally active inhibitors of 5-lipoxygenase. L 691816 can be used for the research of allergies and asthma[1].
Factor B-IN-3 (Example 3 target compound) is a potent complement factor B inhibitor. Factor B-IN-3 can be used for the research of diseases related to inflammation and immunity[1].
Braylin, a coumarin, is a potent phosphodiesterase-4 (PDE4) inhibitor and is involved in anti-inflammatory and immunomodulation, which may serve as a potential target for the study of immunoinflammatory diseases[1].
Felbinac is a potent non-steroidal anti-inflammatory agent, used to treat muscle inflammation and arthritis.
FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].
[D-p-Cl-Phe6,Leu17]-VIP is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP has no activity on glucagon, secretin or GRF receptors[1][2][3].
SPC 839 (compound 10) is an orally active inhibitor of AP-1 and NF-kB mediated transcriptional activation with IC50 of 0.008 μM[1].