Inflammation/Immunology

FABPs ligand 6 (MF6) is an FABP5 and FABP7 inhibitor with K_D values of 874 nM and 20 nM, respectively. FABPs ligand 6 can be used for multiple sclerosis research.

GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC₅₀ values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.

L-NIL is an inducible NO synthase inhibitor, with an IC₅₀ of 3.3 μM for miNOS.

Dauricine, a bisbenzylisoquinoline alkaloid in Menispermum dauricum, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.

Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a K_i of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC₅₀ of 2.1 nM.

Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ～65-fold and ～16-fold selectivitiy for the RARγ (EC₅₀=7.7 nM) over RARα (EC₅₀=500 nM) and RARβ (EC₅₀=125 nM), respectively.

Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells. Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells.

Aminoadipic acid is an orally active lysine oxide derivative. Aminoadipic acid induces ROS generation, increases free Ca²⁺, decreases SOD, and activates TXNIP/NLRP3 pathway. Aminoadipic acid has pro-inflammatory effects. Aminoadipic acid can be used in atherosclerosis research.

(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M₂-selective muscarinic receptor antagonist (pA₂ = 7.86/7.74; pK_i = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M₁ (pA₂ = 6.83/6.36; pK_i = 7.08), the M₃ (pA₂ = 6.92/6.96; pK_i = 6.70) and the M₄ receptors (pK_i = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H₁ receptor antagonist (pA₂ = 7.48).

Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.

Dextran sulfate sodium salt (DSS) (MW 4500-5500) is a polymer of dehydrated glucose with a molecular weight of approximately 4500-5500. Dextran sulfate sodium salt with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 4500-5500) is an inhibitor of complement and coagulation pathways, and belongs to the glycosaminoglycans (GAG) family. Dextran sulfate sodium salt (MW 4500-5500) acts as an anticoagulant, antiviral, and anti-lipemic agent. Dextran sulfate sodium salt (MW 4500-5500) stops HIV-1 virus adsorption to host cells. Dextran sulfate sodium salt (MW 4500-5500) prevents NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 4500-5500) inhibits instant blood-mediated inflammatory reaction (IBMIR).

Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).

Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.

Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice.

Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.

Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC₅₀ of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

CSK-IN-1 (compound 13) is a potent, orally active c-terminal Src kinase (CSK) with IC₅₀ values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. CSK-IN-1 shows the ability to increase T cell proliferation induced by T cell receptor signaling.

AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (K_D = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.