autoimmune disease

ML604440 is a cell permeable proteasome β1i (LMP2) subunit inhibitor.

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.

ML-178, a dichlorobenzene, is a potent and selective agonist of sphingosine-1-phosphate receptor 4 (S1PR4), with an EC50 of 46 nM, and has no effect on other S1P receptors at a concentration of 25 μM.

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

MCC950 (CP-456773) is a NLRP3 inflammasome inhibitor (IC50=7.5-8.1 nM). MCC950 can be used to treat inflammatory diseases, inflammation-related tumors and neurodegenerative diseases.

Ciamexon (Ciamexone) is a novel immunomodulator that has shown promising results in experimental models of autoimmune disease with little demonstrated cytotoxicity.Ciamexon can be used to study endocrine ophthalmopathies and diabetes mellitus, with slight improvement in ophthalmic disease following short-term administration.

Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatment.

Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine, with antiviral efficacy against the chikungunya virus (CHIKV), antimalarial effects, and potential for treating autoimmune diseases.

HPN-01 (IKK inhibitor XII) is a selective IKK inhibitor that inhibits IKK-α, IKK-β, and IKK-ε. HPN-01 reduces the severity of the disease, attenuates the immune imbalance, and prolongs the lifespan of mice in a model of autoimmune encephalomyelitis, and can be used to study immune disorders.

GNE-0946 is an effective and selective RORγ/RORc/NR1F3 antagonist (inverse agonist) with an EC50 of 4 nM in HEK-293 cells. It inhibits IL-17 production in human PBMC cells (IC50 = 17 nM) and can be used in autoimmune disease research.

Nrf2 activator-12 (compound 10v) effectively activates Nrf2 (EC50=83.5 nM) and exhibits favorable pharmacological properties. It reverses disease progression and alleviates demyelination in a mouse model of experimental autoimmune encephalomyelitis.

ERAP1-IN-3 (compound 13) is a potent inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1), with a pIC50 value of 8.6. ERAP1-IN-3 shows potential for research in cancer immunotherapy and autoimmune disease studies.

STAT4-IN-1 is a STAT4 inhibitor with a Ki of 0.35 μM. It holds promise for research into autoimmune diseases, including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes.

TNF-α-IN-24 (Example 15) is a TNF-α inhibitor with an IC50 value of 4.1 nM. It is applicable in research on inflammatory and autoimmune diseases such as rheumatoid arthritis and Crohn's disease.

SCH-900875 is an orally active, brain-penetrant, and selective inhibitor of the CXCR3 receptor, demonstrating significant selectivity towards CXCR1 and CXCR2 receptors as well. By binding to CXCR3, SCH-900875 blocks the ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways and reducing inflammation cell migration. This compound holds potential for research into autoimmune diseases (such as rheumatoid arthritis and multiple sclerosis) and inflammatory conditions (such as psoriasis and inflammatory bowel disease).

IRAK4 modulator-2 (Compound 5) is a selective dual inhibitor of IRAK4 and IRAK1, with IC₅₀ values of 0.005 μM and 0.97 μM respectively. It may be employed in research concerning autoimmune and inflammatory diseases such as rheumatoid arthritis, psoriasis, and inflammatory bowel disease.

Spns2-IN-3 (compound 510) is an SPNS2 inhibitor with an IC50 value of 1.2 μM for hSPNS2. It is applicable in research on autoimmune diseases such as multiple sclerosis (MS) and inflammatory bowel disease (IBD), as well as fibrosis, muscle atrophy, metastasis, acute lung injury, rheumatoid arthritis, colitis, Alzheimer's disease, and other conditions linked to SPNS2 activity.

RORγt inverse agonist 35 (Compound 22) is an RORγt inverse agonist with an IC50 of 1.51 μM. It significantly inhibits Th17 differentiation and pro-inflammatory characteristics in human CD4+ T cells. This compound can be utilized for research on Th17-driven autoimmune diseases, such as psoriasis, multiple sclerosis, and inflammatory bowel disease (IBD).

IRAK4-IN-32 (Compound 10) is a potent inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), with an enzymatic IC50 value of 18.86 nM and a cellular IC50 value of 6.19 nM. It is promising for research in inflammation and autoimmune disease studies.

KBD4466 is a potent oral inhibitor of TLR7 and TLR8, with IC50 values of 0.9 nM and 2.8 nM, respectively. This compound effectively suppresses the inflammatory cytokines IL-6 and IFN-α. KBD4466 has shown to improve disease progression and increase survival rates in the BXSB/MpJ mouse model of systemic lupus erythematosus (SLE). It is suitable for research into autoimmune diseases.

JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 value of 0.15 nM, demonstrating significantly greater inhibitory potency for JAK1 compared to JAK2 and JAK3. It significantly reduces inflammation in ulcerative colitis (UC) mouse models induced by DSS and Crohn's disease (CD) rat models induced by DNBS. JAK1-IN-18 is applicable for research into autoimmune diseases (such as inflammatory bowel disease), viral infections (such as hepatitis B virus infection), and cancers (such as hematologic malignancies).

GCS-12-6 is a potent Th2-selective NKT cell agonist that targets the CD1d protein. It holds potential for research in autoimmune diseases, such as inflammatory bowel disease and multiple sclerosis.

AS2795440 is a PIKfyve inhibitor. It selectively suppresses the production of pro-inflammatory cytokines such as IL-12p40 and IL-6 and the activation of B cells, without affecting Ca2+ signaling. In a mouse model of adjuvant-induced arthritis (AIA), AS2795440 significantly reduces joint inflammation and bone loss. This compound is useful for researching inflammatory and autoimmune diseases like rheumatoid arthritis, psoriasis, and inflammatory bowel disease.