iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology[1].
GSK2263167 is an agonist of S1P1 receptor.
Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)[1].
FK 3311 is a selective inhibitor of COX-2; antiinflammatory agent.IC50 Value: 1.6 uM [1]Target: COX-2Cyclooxygenase (COX) is an intracellular enzyme that converts arachidonic acid into prostaglandin (PG)G2 and PGH2.in vitro: The racemic mixtures and the (R)- and (S)-isomers of the 2 metabolites were inactive in the PGE2 test. IC50 values were more than 100 uM for (2 and 5), compared to 1.6 uM for FK-3311. Antiinflammatory activity was assessed by inhibition of adjuvant-induced arthritis, and analgesic activity was determined in the acetic acid-induced writhing assay. Following p.o. administration of 10 mg/kg, racemic (2) and its optical isomers showed activity comparable to FK-3311 (76% inhibition) in the adjuvant arthritis test, whereas racemic (5) showed very weak activity, and (R)- and (S)-(5) were not tested. With regard to analgesic effects, FK-3311 and racemic (2) showed 81 and 62% inhibitions, respectively, at a dose of 100 mg/kg p.o. The (R)- and (S)-isomers of (2) and racemic (5) all showed 46% inhibition of writhing syndrome. (R)- and (S)-(5) were less active showing 16 and 20% inhibitions, respectively[1].in vivo: L-PVR, CO, PaO(2), and WDR were significantly (P < 0.05) better in the FK group than in the control group. Histological tissue edema was mild, and PMN infiltration was significantly (P < 0.05) reduced in the FK group compared to the control group. The serum TxB(2) levels were significantly (P < 0.05) lower in the FK group than in the control group, while 6-keto-PGF(1alpha) levels were not significantly (P < 0.05) reduced. Two-day survival rate was significantly (P < 0.05) better in the FK group than in the control group [2]. Survival rate was significantly better (p <. 05) and serum GOT levels 30 min after reperfusion were significantly lower (p <. 05) in the FK high-dose group compared to the other two groups. Four hours after reperfusion, GPT levels and liver tissue flow were significantly (p <. 05) better in the FK high-dose group compared to the control. Both 30 min and 4 hr after reperfusion, serum TxB(2) levels were significantly lower in the FK high-dose group compared to the control (p <. 05) [3].
DprE1-IN-1 is a potent DprE1 inhibitor, with ic50 of 10 nM, also inhibits PDE6, with IC50 of 6 uM.IC50 value: 10 nM [1]Target: DprE1in vitro: DprE1-IN-1 demonstrats efficacy in a rodent model of tuberculosis, making it promising for further development.[1]in vivo: The pharmacokinetic profile of DprE1-IN-1 as a representative of the series in mice, rats, and dogs was determined after i.v. and oral dosing. DprE1-IN-1 shows oral bioavailabilities of 86% and 100% in rats and dogs, respectively. The oral exposures of DprE1-IN-1, assessed in infected animals, shows AUCs ranging from 166 to 240 μM · h, and free plasma concentrations were maintained above the MIC for 10 to 24 h. [2]
Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3][4][5].
Ginsenoside Rd2 is a saponin found in Panax japonicus with anti-inflammatory actions[1].
MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR), displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G; showed an IC50 value 39 nM in LANCE® assay of mTOR substrate phosphorylation; dose-dependently inhibits of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473) tumor cell lines harboring mTOR pathway dysregulation with IC50 of <0.12 uM; potently inhibited cell proliferation (IC50 <1 mmol/L) and in vivo tumor growth in multiple NSCLC models of EGFR/T790M, EML4-ALK, c-Met or KRAS (MED <10 mg/kg), also suppressed programmed death ligand 1 (PD-L1) in EGFR- and ALK-driven NSCLC, mediated in part by mTORC2/AKT/GSK3β-dependent proteasomal degradation.
Urolignoside is an antioxidant with free radical scavenging activity. Urolignoside potently scavenges DPPH radical, and exhibits antioxidant to β-carotene-lineoleate model[1].
Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models[1][2][3].
Di-4-ANEPPDHQ, a fluorescent probe for the visualisation of membrane microdomains in living Arabidopsis thaliana cells[1].
SABA1 possesses antibacterial properties against Pseudomonas aeruginosa and Escherichia coli, with an IC50 of 4.0 µM against E. coli ACC[1].
CCR1 antagonist 1 is an antagonist of CCR1, with anti-inflammatory activity.
CORM-3, a water-soluble carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels[1][2][3].
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes[1]. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells[2].
Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research[1][2].
C-176 is a strong and covalent mouse STING inhibitor.
Panaxydiol exhibits histamine-release inhibition activity[1].
Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity[1][2][3][4].
Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α[1].
SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE)[1].
Indoprofen is a non-steroidal anti-inflammatory drug, provide insight into treatments for spinal muscular atrophies.
MRS-1706 is a potent and selective A(2B) adenosine receptor antagonist with a Ki value of 1.39 nM.
RGD peptide acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation[1]. RGD peptides promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing[2][3].
rel-α-Vitamin E (rel-(+)-α-Tocopherol) is a vitamin with antioxidant properties and also a mixture[1].
Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. Target: Histamine H1-receptorMizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat.Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials have shown mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with chronic idiopathic urticaria. Available data also suggest that prophylactic administration of mizolastine is significantly more effective than placebo and as effective as prophylactic terfenadine in delaying the onset of symptoms of seasonal allergic rhinitis.
TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor extracted from patent WO2019220390, compound 2b. TLR7/8-IN-1 can be used for the research of autoimmune disease[1].
Kansuinine E is a plant-derived nitric oxide inhibitor (IC50=6.3 μM). Kansuinine E belongs to jatrophane-type diterpenoids and is isolated from the roots of E. kansui[1].