Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1)[1].
3,5,7-Trimethoxyflavone, a flavonoid compound, can inhibit the TNF-α-induced high expression and secretion of MMP-1 by cells. 3,5,7-Trimethoxyflavone can be used to ameliorate skin damage[1].
Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation[1].
Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
Interleukin II (60-70) is a 60-70 fragment of the cytokine Interleukin II polypeptide[1].
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1][2][3][4].
Cefazolin is an antibiotic used for the research of a number of anti-bacterial infections. Cefazolin can be used for the prophylaxis of surgical antimicrobial. Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD)[1].
Edratide (TV 4710) is a synthetic peptide of 19 amino acid based on the complementarity-determining region 1 (CDR1) of a human anti-DNA antibody that expresses a major idiotype denoted 16/6 Id. Edratide reduces the rates of apoptosis and down-regulates of caspase-8 and caspase-3, up-regulates Bcl-xL. Edratide has the potential for the research of systemic lupus erythematosus (SLE)[1][2][3].
(+)-Balanophonin is a phenolic compound that could be isolated from Passiflora edulis. (+)-Balanophonin possesses anti-oxidant, anticholinesterase, anti-inflammatory, anticancer, and antineurodegenerative activities[1].
8-O-Acetyl shanzhiside methyl ester (ND01) is an iridoid glucoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant in Xi-zang. 8-O-Acetyl shanzhiside methyl ester could inhibt NF-κB.
Peimisine (Ebeiensine) hydrochloride non-competitively antagonizes tracheal smooth muscle muscarinic M receptor and inhibits smooth muscle contraction caused by Ach. Peimisine hydrochloride excits β-receptor, restrains the release of internal calcium, and promotes to releaseing NO in order to relax tracheal smooth muscle and relieve asthma[1].
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA)[1][2].
Regaloside A, a phenylpropanoid, shows significant DPPH radical scavenging activity of 58.0% at 160 ppm. Regaloside A has anti-inflammatory activity[1].
DS28120313 (compound 32) is an orally hepcidin production inhibitor with an IC50 of 0.093 μM[1].
MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies[1][2].
GSK805 is a potent, orally bioavailable RORγγ Inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM[1].
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
KSPWFTTL is an immunodominant Kb-restricted epitope from the p15E transmembrane protein. KSPWFTTL can restore susceptibility of a tumor line to anti-AKR/Gross MuLV cytotoxic T lymphocytes[1][2].
Chamaechromone is a biflavonoid ingredient isolated from the roots of Stellera chamaejasme L. (Thymelaeaceae). Chamaechromone possesses anti-hepatitis B virus (HBV) effects against the surface antigen of HBV (HBsAg) secretion and has insecticidal activities[1].
Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
RXFP1 receptor agonist-6 (Example 7) is a RXFP1 receptor agonist. RXFP1 receptor agonist-6 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 12 nM[1].
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
DPLG3 is a specific chymotryptic-like β5i subunits inhibitor. DPLG3 inhibits mouse i-20S with IC50 of 9.4 nM. DPLG3 can be used for immune disease research[1].
Iodochloromethane-d2 is the deuterium labeled Iodochloromethane[1].
4-Hydroxyacetophenone (P-hydroxyacetophenone) is a key hepatoprotective and choleretic compound in Artemisia capillaris and A. morrisonensis, also has an anti-hepatitis B virus effect and anti-inflammatory effect[1].
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain[1].
Azelastine HCl is a potent, second-generation, selective, histamine antagonist.Target: Histamine ReceptorAzelastine is a selective H(1)-receptor antagonist that inhibits histamine release and interferes with activation of several other mediators of allergic inflammation. Azelastine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine [1]. Topical azelastine progressively improved itching and conjunctival redness in PAC patients compared to placebo and was at least as effective as levocabastine. Rapid relief is consistent with H(1)-receptor antagonist action, while continued improvement up to 6 weeks may be consistent with mechanisms involving other mediators of allergic inflammation [2]. Azelastine nasal spray was reported to control all rhinitis symptoms, including nasal congestion, regardless of rhinitis diagnosis during the 2-week study period. Patients with seasonal allergic rhinitis and patients with seasonal allergic rhinitis plus nonallergic triggers were identified as patient types most likely to respond to azelastine nasal spray [3].