Inflammation/Immunology

EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC₅₀ value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis.

Arctium Seed Extract is obtained from the roots of the burdock plant of the compositae family. It has the effects of antibacterial and anti-inflammatory, detoxification. It can be used in cosmetics material.

dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca²⁺ influx with an IC₅₀ value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal.

DGKα-IN-3 (example 25) is a DGKα inhibitor with the IC₅₀ of 283 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.

Argimesna ethanesulfonate is a uroprotective agent. Argimesna ethanesulfonate is promising for research of hemorrhagic cystitis in cancer chemotherapy.

NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC₅₀s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.

Patchouli alcohol (Standard) is the analytical standard of Patchouli alcohol. This product is intended for research and analytical applications. Patchouli alcohol is a natural tricyclic sesquiterpene, exhibits anti-Helicobacter pylori, anti-inflammatory and antioxidant properties.

HPK1-IN-58 (Compound 26) is an inhibitor of HPK1 (IC₅₀: 2.6 nM) and SLP76 (IC₅₀: 20 nM). HPK1-IN-58 enhances IL-2 secretion and reverses PGE2-induced immunosuppression. HPK1-IN-58 can be used in anti-tumor immunity research.

PADI4-IN-1 is a potent peptidylarginine deiminase isoform 4 (PADI4) inhibitor with an IC₅₀ of 1.5 μM and SI (PADI1/PADI4) of 52.1. PADI4-IN-1 can inhibit cellular citrullination events. PADI4-IN-1 can be used for the research of inflammation, such as rheumatoid arthritis.

Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

Keap1-Nrf2-IN-6 (compound 64) is a potent and selective Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC₅₀ of 41 nM, K_d of 68 nM.

(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.

Etiprednol dicloacetate (BNP 166) is an anti-inflammatory agent. Etiprednol dicloacetate inhibits eosinophil accumulation. Etiprednol dicloacetate can be used in the research of inflammatory airway diseases, such as asthma.

COX-2/Aromatase-IN-2 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-2 can simultaneously inhibit COX-2 and aromatase, suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-2 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-2 can be used for the study of inflammation and breast cancer.

GSK5784283 (SHR-1905) is a bivalent antibody against TSLP, which is applicable to research related to asthma. GSK5784283 has two Fab arms and is a humanized IgG1κ monoclonal antibody. GSK5784283 effectively reduces the levels of eosinophils, FeNO, TARC and eotaxin-3. GSK5784283 regulates FEV1 (forced expiratory volume in one second).

CSLP37 is a selective RIPK2 inhibitor with an IC₅₀ of 16.3 nM. CSLP37 shows no inhibitory activity against RIPK1 and RIPK3. CSLP37 displays potent suppression of cellular NOD1 and NOD2 responses.

QX-31 is an orally active selective NLRP3 inhibitor with a K_d value of 2.8 μM for hNLRP3. QX-31 inhibits PI3K/AKT and HIF-1α signaling. QX-31 shows anti-fibrotic effects in mouse models of unilateral ureteral obstruction and ischemia-reperfusion injury. QX-31 can be used for research on renal fibrosis.

LEESGGGLVQPGGSMK TFA, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK TFA can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.

PI3Kδ-IN-28 is an orally active and selective PI3Kδ inhibitor with an IC₅₀ of 6.1 nM. PI3Kδ-IN-28 inhibits pro-inflammatory M1 macrophage polarization, promotes anti-inflammatory M2 phenotype, and alleviates pulmonary edema and inflammatory infiltration. PI3Kδ-IN-28 is applicable to research related to acute lung injury.

QC-308 hydrochloride is a HO-1/HO-2 inhibitor, with an IC₅₀ of 0.27 μM against rat HO-1 and an IC₅₀ of 0.46 μM against rat HO-2. QC-308 hydrochloride inhibits the activities of rat HO-1 and HO-2 in carbon monoxide generation assays using spleen and brain microsomes, respectively. QC-308 hydrochloride also exhibits senolytic activity, reducing the survival rate of adipogenic progenitor cells in skeletal muscle fibers of senescent mice and human skeletal muscle myoblasts. QC-308 hydrochloride is applicable for senescence-related research.