immune

Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

Taurochenodeoxycholic Acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid.

Pyrroloquinoline quinone (PQQ), as a well-known redox enzyme cofactor, PQQ can protect NS/PCs against glutamate toxicity associated with ROS-mediated mitochondrial pathway,

Pyrroloquinoline quinone disodium salt (Methoxatin disodium salt), an aromatic tricyclic o-quinone, is a redox cofactor for bacterial dehydrogenases. It is an efficient electron transfer catalyst from a number of organic substrates to molecular oxygen (O2), constructing quinoprotein model reactions.

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.

SM-276001 is a potent, selective agonist of TLR7 and an orally active interferon (IFN) inducer.

3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.

7α,25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist, as well as an endogenous ligand, of the orphan GPCR receptor EBI2 (GPR183). It serves as a chemokine directing the migration of B cells, T cells, and dendritic cells and exhibits high potency in activating EBI2 (EC50=140 pM; Kd=450 pM) [1][2].

N-Hydroxypipecolic acid (NHP) is a plant metabolite and a systemic acquired resistance (SAR) regulator.

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor that inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. It blocks the synergy between NOD2 and TLR2 without affecting NOD1, TNFR1, and TLR2-mediated responses. At 5 μM, GSK717 inhibits the release of IL-8, IL-6, TNFα, and IL-1β in primary human monocytes stimulated with MDP[1]. [1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

BMS-1166 is a potent inhibitor of the PD-1/PD-L1 interaction.

AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.

GPR34 receptor antagonist 2 (Tyrosine, N-[(2E)-3-(4'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)-) is an anti-inflammatory agent.

CID44216842 (KUC103479N-02) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 receptor-associated kinase-4 (IC50 = 4 μM).

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Lipopolysaccharides (LPS), derived from Escherichia coli O55:B5, are essential components of the outer membrane of Gram-negative bacteria. Composed of lipid A, a core oligosaccharide, and an O-specific polysaccharide, LPS exhibits strong immunogenicity. It activates immune cells via the TLR4 receptor, induces chemotactic cell migration and cytokine secretion, and helps maintain the integrity of the bacterial outer membrane, protecting against bile salts and lipid-based antibiotics. LPS is commonly used to establish inflammatory models, including arthritis, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome (ARDS), and gastrointestinal disease models.