Inflammation/Immunology

L-Lysine-¹³C₆,¹⁵N₂ (hydrochloride) is the ¹³C- and ¹⁵N-labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.

PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) that can cross the blood-brain barrier, with an EC₅₀ of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.

Sappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular .

SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC₅₀ value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration.

CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC₅₀ =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC₅₀ of 4.2 μM. Potential anti-metastasis Agent.

Gracillin is a steroidal saponin that can be extracted from the roots of the plant and has anti-tumor properties. Gracillin can induce cancer cell apoptosis and autophagy.

Dendrobine is an alkaloid isolated from Dendrobium nobile. Dendrobine possesses antiviral activity against influenza A viruses, with IC₅₀s of 3.39 μM, 2.16 μM and 5.32 μM for A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2), respectively. Dendrobine activates the JNK/p38/Nrf2 signaling pathway. Dendrobine exhibits antiviral, antitumor, anti-inflammatory, and neuroprotective properties.

Leonurine hydrochloride is an alkaloid isolated from Leonurus artemisia, with anti-oxidative and anti-inflammatory.

LEAP-2 (Human liver expressed antimicrobial peptide-2) is a GHS-R1a antagonist, with an IC₅₀ of 6.0 nM. LEAP-2 suppresses the orexigenic effect of ghrelin. LEAP-2 attenuates ghrelin-induced growth hormone (GH) release and reduces basal food intake. LEAP-2 exhibits antimicrobial activity against microbial model organisms. LEAP-2 can be used for the study of obesity and infection.

Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC₅₀ of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.

ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC₅₀ of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).

GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.

CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC₅₀ values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC₅₀ of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.

AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).

Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.

Ibuprofen ((±)-Ibuprofen) sodium is an orally active, selective COX-1 inhibitor with an IC₅₀ value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.

Trimethylamine N-oxide-d₉ is the deuterium labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

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.

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.

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.