YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively[1].
Influenza virus-IN-2 (compound 19) is a potent influenza virus inhibitor with an EC50 of 2.58 µM and CC50 of 150.85 µM. Influenza virus-IN-2 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 489.39 nM. Influenza virus-IN-2 shows shows anti-influenza A virus activities[1].
DSP Crosslinker is a cleavable ADC linker, used in the synthesis of antibody-drug conjugates (ADCs)[1].
Feretoside, a phenolic compound extracted from the barks of E. ulmoides, is a HSP inducer which act as cytoprotective agent.
AJ2-71 is a SLCl5A4 inhibitor. AJ2-71 inhibits IFN-α production. AJ2-71 blocks SLC15A4-mediated MDP transport. AJ2-71 can be used for research of inflammation[1].
Triptoquinone H is a class of natural product isolated from traditional Chinese medicine Tripterygium hypoglaucu. Triptoquinone H has strong cytotoxic, immunomodulatory and anti-inflammatory activities. Triptoquinone H can be used for cancer or inflammatory diseases research[1].
Edicotinib is a selective and orally available colony-stimulating factor-1 (CSF-1) receptor inhibitor, and has entered phase IIA clinical trial to study rheumatoid arthritis (RA) despite disease.
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice[1][2].
Angeloylbinankadsurin A (compound 7) is an anti-rheumatoid arthritis (RA) agent that can be isolated from EtOAc and CH2Cl2 extracts of Black Tiger Beard. Angeloylbinankadsurin A exhibits inhibitory activity on RA-FLS cells (IC50=11.70 μM). Angeloylbinankadsurin A is slightly toxic to human cancer cell lines (Hela and BGC-823) (IC50=19.9 μM, 21.93 μM)[1].
Pumaprazole is a reversible proton pump antagonist.
Methyl(E)-cinnamate-d7 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
Bucloxic acid is an anti-inflammatory pyrrazole derivative. Bucloxic acid can be used in the treatment of chronic glomerular nephropathies.
Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.Target: Histamine H1 ReceptorDesloratadine binds to the human H1 receptor with Ki value of 0.87 nM in displacing tritiated mepyramine. Desloratadine (100 nM to 10 μM) inhibits both IgE-mediated and non-IgE-mediated generation of the cytokines IL-4 and IL-13 by human basophils. Desloratadine (300 nM to 100 μM) inhibits both IgE and non-IgE-mediated histamine release from human peripheral blood basophils. Desloratadine (0.1 μM to 10 μM) is also shown to inhibit platelet-activating factor-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion in eosinophils obtained from patients with allergic rhinitis or allergic asthma [1]. Desloratadine (1 μM-10 μM) dose-dependently inhibits the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μM-10 μM) dose-dependently inhibits IL-13 secretion from basophils activated with IL-3 and PMA from human basophils. Desloratadine (10 μM) pretreatment results in a substantial decrease of the induced cytokine message in cultured basophils. Desloratadine (10 μM) pretreatment causes approximately an 80% reduction in the IL-4 message accumulated with anti-IgE activation in cultured basophils. Desloratadine (10 μM) also inhibits the histamine and IL-4 protein secreted into the supernatants of cultured basophils [2]. [3H]Desloratadine binds to the human histamine H1 receptor expressed in CHO cells with Kd of 1.1 nM. Desloratadine is 52, 57, 194, and 153 times more potent than cetirizine, ebastine, fexofenadine, and loratadine, respectively, in competition-binding studies [3].
Bay 65-1942 free base is an ATP-competitive and selective IKKβ inhibitor.
PIPES (1,4-Piperazinediethanesulfonic acid) disodium is an important component of PIPES buffer agent used in biochemistry[1].
Echinatin is a chalcone isolated from the Chinese herbal medicine Gancao with hepatoprotective and anti-inflammatory effects. Echinatin may undergo an electron transfer (ET) and a proton transfer (PT) to cause the antioxidant action in aqueous solution[1]. Echinatin can be quickly absorbed and eliminated and extensively distributed with an absolute bioavailability of approximately 6.81% in Rat[2].
PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator[1].
Caryophyllene oxide, isolated from from Annona squamosa L. bark., possesses analgesic and anti-inflammatory activity[1].
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities.
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases[1].
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19[1][2][3].
Azido-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as the conjugate CPT-APO (CPT: Camptothecin (HY-16560)).
Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor[1].
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA)[1].
Allopurinol sodium is a potent xanthine oxidase inhibitor (IC50 values of 0.2 to 50 μM). Allopurinol sodium can be used for the research of hyperuricemia and gout. Antileishmanial effect[1][2].
COX-2-IN-19 (Compound 24) is a potent COX-2 inhibitor with an IC50 of 1.76 μM. COX-2-IN-19 shows in vivo anti-inflammatory activity[1].
DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.
NecroX-5 is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.
Apremilast D5 (CC-10004 D5) is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
Hydroxyzine is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 ?M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 ?g/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].