Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor[3] properties[1]. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways[2]. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells[3].
Tolfenamic Acid-D4 (GEA 6414-D4) is the deuterium labeled Tolfenamic Acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1[1][2].
Sodium Sulphanilate is a biochemical indice of inflammation-associated acute-phase response[1].
Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
Sinulatumolin C (compound 3) is an anti-inflammatory agent. Sinulatumolin C has significant TNF-α inhibitory activity with an IC50 value of 2.6 μM[1].
IQ-1 is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1 has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
Dimethindene maleate is a selective histamine H1 antagonist with antihistamine effects. Dimethindene maleate can be used for the research of hypersensitivity reactions[1][2][3].
FKK is an indazole derivative and also a novel bronchodilator.
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580. IC50 value: 44 nM ( p38α)Target: p38 MAPKSB 239063 reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo.
A potent TLR7 agonist with EC50 of 59 nM.
Goflikicept (RPH 104) is a hybrid protein that selectively binds and inactivates both circulating IL-1ß and IL-1α. Goflikicept has the potential for the research of ST-segment elevation myocardial infarction (STEMI)[1].
IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
YM158 free base is a potent and selective LTD4 and TXA2 receptor antagonist with pA2 values of about 8.87 and 8.81, respectively.
TC-E 5003 is a selective PRMT1 inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 has anti-inflammatory properties in TLR4 signaling[1][2].
7β-Hydroxy-epi-androsterone (7β-Hydroxy-EpiA) can bind to ERβ and has anti-inflammatory and neuroprotective properties. 7β-Hydroxy-epi-androsterone is an endogenous androgenic derivative of dehydroepiandrosterone[1][2][3].
S 16474 is an antagonist of Neurokinin-1 Receptor.
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity[1].
Jedi2 is a Piezo1 channel activator, but no specific Piezo2 activators. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770 μM[1].
GSK-7975A is a potent and orally available CRAC channel inhibitor.
BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1]Target: Factor D; C1sBCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX 1470(Thrombin inhibitor) blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat.
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent[1].
Rabeprazole sodium(LY307640 sodium) is an antiulcer drug in the class of proton pump inhibitors.Target: Proton PumpRabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H+/K+ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfenamide. When studied in vitro, rabeprazole is chemically activated at pH 1.2 with a half-life of 78 seconds.
Manfidokimab (AK120) is an anti-interleukin 4 receptor alpha (IL-4Rα) IgG4 monoclonal antibody[1].
Methylsyringin exhibits anti-inflammatory activity in the LPS-stimulated RAW264.7 cells.
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production[1].
β-Interleukin I (163-171), human, an immunostimulatory fragment of human IL-1β peptide, is a T cell activator. β-Interleukin I (163-171), human is not an IL-1R-binding domain of IL-1β. β-Interleukin I (163-171), human is a potent adjuvant that enhances the immune response in a variety of exptl. situations[1][3][4].
Rhein is a lipophilic anthraquinone extensively found in medicinal herbs, and has many pharmacological effects, including epatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities. IC50 value:Target:In vitro: Rhein (0.1 and 1 mg/mL) evidently suppressed cell proliferation and mitogen-activated protein (MAP) kinase activation in human colon adenocarcinoma cells (Caco-2) but significantly lessened H2O2-induced DNA damage and the elevated MDA and ROS levels induced by H2O2/Fe2+ at the concentrations of 0.1–10 mg/mL [1].In vivo: Oral administration of rhein (150 mg/kg/d) evidently ameliorated renal interstitial fibrotic lesions and attenuated the expression of α-SMA and deposition of fibronectin (FN) in mice with renal interstitial fibrosis induced by unilateral ureteral obstruction. Rhein also suppressed TGF-β1 and its type I receptor expression in obstructed kidneys [1]. The biochemical parameters results of IgAN model rats showed that rhein-prevented and rhein-treated both improved the biochemical parameters and relieved renal pathological injury. The expressions of renal tissue TLR4, TGF-β1, but not TLR9 were significantly elevated in IgAN model rats (P < 0.05). Rhein-prevented and rhein-treated both inhibited TLR4 and TGF-β1 expressions [2].
UC-1V150 is a specific TLR7 (Toll-like receptor) agonist that stimulates cellular immune responses and has anti-tumor activity. UC-1V150 can be used to synthesize ISAC (Immune-Stimulating Antibody Conjugates) molecule[1][2].
p38 MAPK-IN-4 (compound 6) is a p38 MAPK inhibitor with an 50 of 35 nM[1].
THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma[1][2].