Helenalin acetate, a natural NF-κB inhibitor, is a potent C/EBPβ inhibitor. Helenalin acetate has anti-inflammatory and anticancer activities[1].
RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphan receptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer[1].
Phosphoramidon, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively[1][2][3].
4'',5''-Dehydroisopsoralidin is a β-glucuronidase inhibitor (IC50: 6.3 μM). 4'',5''-Dehydroisopsoralidin has anti-inflammatory and anti-oxidative effects. 4'',5''-Dehydroisopsoralidin can be used in the research of inflammation and cancners[1][2].
Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders[1].
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3].
Lysophosphatidylcholines are a class of chemical compounds which are derived from phosphatidylcholines. Lysophosphatidylcholine is produced from phospholipids by the action of phospholipase A2 (PLA2). Lysophosphatidylcholine plays critical role in allergic airway disease manifestation[1].
Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.
Mizolastine dihydrochloride 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.
Trihydroxycholestanoic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Refsum Disease, D Bifunctional Protein Deficiency and Infantile Refsum Disease[1][2][3][4].
Thymus factor X is a biologically active polypeptide which can be used as a natural stimulator of lymphocyte function.
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis[1].
Immune cell migration-IN-2 is a potent immune cell migration inhibitor with an EC50 of 13.5 nM in a T-cell adhesion assay. Immune cell migration-IN-2 is extracted from patent WO2019001171, example 11, can be used for dry-eye and other retinal diseases research[1].
GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models[1].
AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model[1].
PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively[1].
Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.
CXCR4-IN-1 (Example C5) is a CXCR4 inhibitor (IC50: 20 nM). CXCR4-IN-1 can be used for research of cancer, HIV, diabetic retinopathy, inflammation, etc[1].
Tetroxoprim is an antimicrobial DHFR inhibitor[1].
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders[1].
Norbraylin, a natural prenylated coumarin, is a PDE4D2 inhibitor with an IC50 value of 7.15 μM[1].
IDE1 is an inducer of definitive endoderm 1 (IDE1).
MPO-IN-4 (compound 12) is a potent and selective myeloperoxidase (MPO) inhibitor with an IC500 of 25 nM. MPO-IN-4 has no effect on methyl guanine methyl transferase (MGMT)[1].
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM[1]. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC)[2].
G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer[1].
DOTA-biotin is a DOTA-based small molecule hapten. DOTA-biotin has low tissue and whole-body retention in mice 4 h postinjection[1].
Fibronectin, a glycoprotein (~500 kDa) present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans[1].
BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3[1].