BT-11 is an orally available LANCL2 binding compound for treating inflammatory bowel disease.
Cyclosporin U (SMP0V32C6L) is an cytostatic agent that plays an important role in preventing rejection of transplanted organs[1].
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases[1].
Homomangiferin, isolated from the leaves of M. indica L., is mangiferin monomethyl ether. Homomangiferin has important medicinal properties and is widely used to relieve many symptoms, for example coughing and asthma[1].
Propacetamol is a water-soluble acetaminophen precursor drug, which can be administered via non intestinal route. It is an analgesic used to treat postoperative pain, acute trauma and gastrointestinal disorders[1].
10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations[1][2].
Bersiporocin is a prolyl-tRNA synthetase inhibitor. Bersiporocin has an IC50 of ≤100 nM for phosphoribosylpyrophosphate synthetase (PRS). Bersiporocin can be used for the research of antifibrotic[1][2].
Minecoside is a CXCR4/STAT3 inhibitor with anticancer and anti-inflammatory activity. Minecoside decreases CXCR4 expression and suppresses STAT3 activation, thus to inhibit CXCL 12-induced invasion. Minecoside potently inhibits cancer metastasis and promotes apoptotic progression[1][2].
ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects[1][2].
AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity[1]. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice[2].
Kisspeptin-10, rat is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10, rat is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound[1].
Indomethacin-D4 (Indometacin-D4) is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1].
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].
Tolmetin-d3 is the deuterium labeled Tolmetin. Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research[1] [2] .
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
ω-Conotoxin SO3 is a blocker of N-type voltage-sensitive calcium channel. ω-Conotoxin SO3 is an analgesicω-conotoxin that can be isolated from the venom of C. striatus[1][2].
CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions[1].
ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
SLF1081851 (16 d) is an effective Sphingolipid Transporter 2 (Spns2) (S1P transporter) inhibitor with an IC50 value of 1.93 μM (S1P), SLF1081851 inhibits SphK2 with an IC50 value of ≈ 30 μM (SphK2), and is at least 15-fold more selective for SphK2 than SphK1. SLF1081851 has the potential to investigate Spns2 biology and can be used for autoimmune encephalomyelitis (EAE) research[1].
Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities[1], act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM[2].
PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research[1].
VGX-1027(GIT27) is an isoxazole compound that exhibits various immunomodulatory properties; reduce the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages.IC50 value: Target: immunomodulatorAdministration of VGX-1027 to NOD mice with spontaneous or accelerated forms of diabetes induced either by injection of cyclophosphamide or by transfer of spleen cells from acutely diabetic syngeneic donors markedly reduced the cumulative incidence of diabetes and insulitis. In addition, VGX-1027 given either i.p. or p.o. to CBA/H mice made diabetic with multiple low doses of streptozotocin successfully counteracted the development of destructive insulitis and hyperglycemia [1]. VGX-1027 appeared to spare T cell function as it was unable to modify the proliferation and/or secretion of IL-2, IFN-gamma and IL-4 induced in purified murine CD4+ T cells from stimulation with either CD3+CD28 or ConA [2]. VGX-1027 inhibited both proliferation of enterobacterial antigen-reactive CD4+CD25- T cells in vitro and the development of clinical and histological signs of colitis in vivo [3].
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM)[1][2].
Prednisolone disodium phosphate is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorPrednisolone irreversibly binds with glucocorticoid receptors (GR) alpha and beta for which they have a high affinity. Prednisolone can activate and influence biochemical behaviour of most cells. The steroid/receptor complexes dimerise and interact with cellular DNA in the nucleus, binding to steroid-response elements and modifying gene transcription. They induce synthesis of some proteins, and inhibit synthesis of others. Prednisolone exerted a delayed biphasic effect on the resistant CCRF-CEM leukemic cell line, necrotic at low doses and apoptotic at higher doses. At low doses, prednisolone exerted a pre-dominant mitogenic effect despite its induction on total cell death, while at higher doses, prednisolone's mitogenic and cell death effects were counterbalanced [1, 2].
7β-Hydroxycholesterol is an oxysterol that derived by the oxidation of cholesterol. 7β-hydroxycholesterol is a powerful inducer of oxidative stress, inducing dysfunction of organelles (mitochondria, lysosomes and peroxisomes) that can cause cell death[1].
Blood group A pentasaccharide (A-Pentasaccharide), an oligosaccharide in urine, can inhibit the binding of anti-A antibody to blood group A substance[1].
Yakuchinone A is a natural product isolated from the fruit of Alpinia oxyphylla, which can induce apoptosis and has anticancer and anti-inflammatory activities[1].