MCC950 sodium is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
AZD3264 is a selective IkB-kinase IKK2 inhibitor.
Seclazone is a heterocyclic compound, possesses anti-inflammatory, analgesic, antipyretic and diuretic properties. Seclazone is orally bioavailable[1].
CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
D-α-Hydroxyglutaric acid ((R)-2-Hydroxypentanedioic acid) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling[1][2][3][4][5].
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research[1][2].
Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect[1].
Sodium gualenate (Guaiazulenesulfonate sodium) is a hydrophilic derivative of guaiazulene with excellent anti-inflammatory and wound-healing effects mainly used for the treatment of duodenal ulcer, gastric ulcer and gastritis.
Tyk2-IN-13 (compound 30) is an orally active TYK2 inhibitor. Tyk2-IN-13 inhibits IFNα stimulated STAT3 phosphorylation with an IC50 value of 1.90 nM. Tyk2-IN-13 can be used for the research of autoimmune diseases[1].
Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.IC50 value: 32 uMTarget: H1-receptorLoratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells.
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype[1].
Fenamic acid is a chloride channel blocker[1].
Bromhexine is a potent expectorant. Bromhexine increase mucociliary clearance and reduces cough. Bromhexine can be used in study various respiratory diseases[1].
Toddacoumalone is a natural inhibitor of phosphodiesterase 4 (PDE4) with moderate potency and imperfect drug-like properties. Toddacoumalone has the potential for the research of inflammatory diseases such as psoriasis[1].
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays sedative, antiserotonin, antispasmodic, and antiemetic properties[1][2].
Flo8 is a potent anti-inflammatory and antioxidant compound. Flo8 inhibits the release of intracellular reactive oxygen species (ROS) and nitric oxide (NO) and suppresses neuronal apoptotic by inhibiting inflammatory and apoptotic signaling pathways. Flo8 can be used for Parkinson's Disease (PD) research[1].
Chrysanthemol is a trans-eudesmane type sesquiterpene that can be isolated from Chrysanthemum indicum. Chrysanthemol has anti-inflammatory activity[1].
MG-262 is a reversible proteasome inhibitor with diverse biological activities[1][2][3].
RXFP1 receptor agonist-3 (Example 223) is a RXFP1 receptor agonist. RXFP1 receptor agonist-3 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 2 nM[1].
1,4-Cineole is a widely distributed, natural, oxygenated monoterpene[1]. 1,4-Cineole, present in eucalyptus oil, activates both human TRPM8 and human TRPA1[2].
Ebastine-d5 (LAS-W 090-d5) is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1][2].
Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
Balsalazide-d4 is deuterium labeled Balsalazide. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Astemizole, a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has anticholinergic and antipruritic effects[1][2].
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases[1]. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
RXFP1 receptor agonist-7 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-7 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.2 nM[1].
rel-Paroxetine hydrochloride is a isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
Ex26 (S1P1-IN-Ex26) is a potent and selective Sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach[1].
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity[1][2][3].