Icosabutate, a structurally engineered and orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis[1]. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia [2].
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia[1].
Enterobactin is a bacterial siderophore that promotes iron absorption and can be used to study inflammation. Enterobactin also disrupts macrophage (MΦs) iron homeostasis and M1/M2 polarization to protect intracellular bacteria from host antimicrobial effects[1].
Fluticasone propionate-d5 is deuterium labeled Fluticasone (propionate). Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (KD) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity[1][2].
A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively; >15-fold selectivity for TRPV4 over TRPV1, TRPV3 and TRPM8, and a panel of 54 other common biological targets.
Saucerneol is a lignans that can be isolated from Saururus chinensis. Saucerneol inhibits LPS-induced or Con A-induced lymphocytes proliferation. Saucerneol inhibits mixed lymphocyte response. Saucerneol also inhibits mitogens-induced cytokines secretion[1].
J-113863 is a potentand selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 has no active against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3].
c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM.c-Fms-IN-10 has anti-tumor activity[1].
Prednisolone 21-acetate is an adrenal cortico hormones, with anti-inflammatory, anti-allergic and immune suppressive effects.
Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1 (PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer[1].
Kansuinine B inhibits IL-6-induced Stat3 activation. Kansuinine B possesses anti-viral activity and could be used in the study for COVID-19[1][2][3].
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
Benzothiazole is a natural occurring heterocyclic nuclei. Benzothiazole nucleus possesses a number of biological activities such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, antiviral, antileishmanial, and antiviral[1].
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1)[1].
cFMS Receptor Inhibitor IV (Compound 42) is a potent cFMS inhibitor with an IC50 of 0.017 μM[1].
Homocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects[1].Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation[2].
WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).EC50 value: 28 nM [1]Target: β cell proliferation agonistProtocol(Only for Reference) [1]In vivo efficacy studies in RIP-DTA mice:RIP-DTA mice were purchased from Jackson Laboratories and all aspects of their treatment were outlined in a protocol approved by an internal animal care and use committee (IACUC). Mice were housed as 3-5 mice per cage and fed standard chow and water. During disease induction, doxycycline was added to the drinking water at a concentration of 2 mg/mL. Animals were injected intraperitoneally with saline-formulated WS6 at 5 mg/kg once every other day (for efficacy study). Blood glucose was monitored every third day. Mice were sacrificed at the end of week 1 and pancreas was fixed in formalin, sectioned, and stained for Ki67 and insulin. At the end of week 6, wet pancreas weight was recorded, and fixed pancreata were sectioned and stained for insulin; total insulin area and wet weight were used to calculate beta cell mass. For pharmacokinetic studies, WS6 was formulated at 50 mg/kg and given as single intraperitoneal dose, followed by serum collection and analysis of compound concentration in serum to determine CMAX and half-life (T1/2).
HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-14 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 79) [1].
Homobutein a natural chalcones (can be found in many medicinal plants, fruits, vegetables, spices and nuts), is a potent HDACs/NF-κB dual inhibitor with IC50s of 190 and 38 μM, respectively. Homobutein also a chelator of iron (II and III) cations, shows various activities, including anticancer, anti-inflammatory, antiparasite and antioxidation[1][2][3][4].
4'-Methoxyisoagarotetrol is chromone derivative and shows moderate PDE?3A inhibitory activity (IC50=54 μM)[1].
Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation
Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities[1].
N4-Acetylcytidine triphosphate is a endogenous nucleoside metabolite from the degradation of tRNA, primes and activates NLRP3 inflammation by inducing HMGB1 expression[1].
3,4-O-Isopropylidene-shikimicn acid is a natural product that can be isolated from the whole plants of Hypericum wightianum. 3,4-O-Isopropylidene-shikimic acid has anti-inflammatory effect and antioxidant activities[1][2].
MRGPRX4 agonist-1 (compound 30d) is a selective agonist of MRGPRX4 with EC50s of 11.2 nM and 30.0 nM in Ca2+ and β-arrestin experiments, respectively[1].
Lewis X trisaccharide (Lewis X, Lex) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis[1][2][3].
ACAT-IN-9 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 207. ACAT-IN-9 inhibits NF-κB mediated transcription[1].
Quetmolimab is a humanized anti-CX3CL1 monoclonal antibody. However, CX3CL1 is a chemokine with a modulating effect on chemotaxis and adhesion[1].
Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
STING agonist-11 (Compound 92) is a potent small molecule cyclic urea activator of STING with EC50 of 18 nM. Activation of STING is a highly promising approach in immunotherapy[1].