Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3][4][5].
Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models[1][2][3].
Di-4-ANEPPDHQ, a fluorescent probe for the visualisation of membrane microdomains in living Arabidopsis thaliana cells[1].
SABA1 possesses antibacterial properties against Pseudomonas aeruginosa and Escherichia coli, with an IC50 of 4.0 µM against E. coli ACC[1].
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes[1]. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells[2].
C-176 is a strong and covalent mouse STING inhibitor.
Panaxydiol exhibits histamine-release inhibition activity[1].
Fluocinolone Acetonide is a glucocorticoid derivative used topically in the treatment of various skin disorders.Target: Glucocorticoid ReceptorFluocinolone acetonide is a corticosteroid primarily used in dermatology to reduce skin inflammation and relieve itching. It is a synthetic hydrocortisone derivative. The fluorine substitution at position 9 in the steroid nucleus greatly enhances its activity. A typical dosage strength used in dermatology is 0.01-0.025%. One such cream is sold under the brand name Flucort-N and includes the antibiotic neomycin. The Glucocorticoid Receptor(GR) binding affinity (IC50) for Fluocinolone Acetonide(FA) was 2.0 nM, respectively. The values is similar to the GR transactivation EC50 of 0.7 nM for FA, respectively [1, 2].
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. ROCK-IN-6 is extracted from patent WO2021164351 A1, example 7, has the potential for glaucoma and retinal diseases research[1].
Kalii Dehydrographolidi Succinas (Potassium dehydroandrographolide succinate), extracted from herbal medicine Andrographis paniculata (Burm f) Nees, is widely used for the treatment of viral pneumonia and viral upper respiratory tract infections because of its immunostimulatory, anti-infective and anti-inflammatory effect[1][2].
Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity[1][2].
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
Begelomab (SAND-26) is a murine IgG2b monoclonal antibody against DPP-4/CD26. Begelomab can be used for the research of severe refractory idiopathic inflammatory myopathy[1][2].
HS220 (HS-220) is a Plasmodium-selective takinib analog that targets atypical P. falciparum protein kinase 9 (PfPK9, Kd=4.1 uM) but does not inhibit HsTAK1, decreases K63-linked ubiquitination in P. falciparum; inhibits P. berghei parasite load in HuH7 cells with EC50 of 43 uM, with no significant change on HuH7 viability; induce a unique phenotype where parasite size in hepatocytes increases.
Bermekimab (MABp1) is a human monoclonal antibody that targets interleukin-1alpa (IL-1α). Bermekimab prevents tumour-related inflammation[1].
Anti-inflammatory agent 46 (compound 7h) is an anti-inflammatory agent with nitric oxide (NO) inhibitory effect. Anti-inflammatory agent 46 binds to iNOS with low energies, inhibits swelling in mice (at dose of 10 mg/kg)[1].
c-JUN peptide is a cell-permeable c-JUN-JNK interaction inhibitor. c-JUN peptide inhibits serum-induced c-Jun phosphorylation. c-JUN peptide induces apoptosis[1].
SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).IC50 value:Target: p38 MAPK inhibitorin vitro: SKF-86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC50 120 microM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM) and its sonicate (IC50 100 microM) and human monocytes (IC50 1 microM). In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM) [1]. differentiation of HL-60 cells toward the neutrophil phenotype resulted in a loss in c-Jun NH2-terminal kinase activation with concomitant acquisition of formylmethionylleucylphenylalanine-stimulatable and stress-inducible p38 MAPK activity as well as apoptosis blockade by SKF-86002 [2]. SKF-86002 blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP [3].
12-Epinapelline is a diterpene alkaloid isolated from Aconitum baikalense. 12-Epinapelline exhibits Anti-inflammatory activity and stimulates the growth of colonies from fibroblast precursors[1][2].
RXFP1 receptor agonist-5 (Example 98) is a RXFP1 receptor agonist. RXFP1 receptor agonist-5 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1.3 nM[1].
10-Hydroxy-2-decenoic acid (10-HDA) is the major lipid component of royal jelly produced by honeybees. 10-Hydroxy-2-decenoic acid has several health-beneficial effects in mammals, such as antitumor activity, anti-inflammatory activity, and antiangiogenic activity. 10-Hydroxy-2-decenoic acid also extends the lifespan of C. elegans[1].
IKK2-IN-3 (Compound 8) is an IKK2 inhibitor with an IC50 of 0.075 μM[1].
STING agonist-10 (Compound 91) is a potent small molecule cyclic urea activator of STING with the EC50 of 2600 nM. Activation of STING is a highly promising approach in immunotherapy[1].
WKYMVM (TFA) is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase[1][2].
Massonianoside B is an antioxidant, which can be isolated from Cedrus deodara pine needle. Massonianoside B exhibits radicals scavenging capacities, and restores CCL4-impaired activity of antioxidant enzymes[1].
(+)-Pinoresinol diacetate is an antifungal agent that can be isolated from Sambucus williamsii[1].
Linderene acetate, isolated from the root of Lindera strychnifolia, is a prolyl endopeptidase inhibitor[1].
(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research[1][2].
ODN 24987 is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’[1].