glomerulonephritis

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity used in treating tumors, immune system disorders, and blood and lymphatic system disorders. Additionally, Edralbrutinib is studied for its efficacy in membranous glomerulonephritis and optic neuromyelitis optica.

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1 NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

CT52923 is a selective, orally active antagonist of platelet-derived growth factor receptor (PDGFR), functioning as an ATP-competitive inhibitor. It has versatile applications for researching pathological diseases such as atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer.

CK2-IN-4 is a protein kinase (CK2) inhibitor with an IC50 value of 8.6 µM. CK2-IN-4 has potential anticancer ah and anti-inflammatory activity for the study of viral infections and glomerulonephritis diseases.

High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J.Hepatol. 42 850 PMID:15885356 |Ma et al (2007) A pathogenic role for c-Jun amino-terminal kinase signaling in renal fibrosis and tubular cell apoptosis. J.Am.Soc.Nephrol. 18 472 PMID:17202416 |Ma et al (2009) Blockade of the c-Jun amino terminal kinase prevents crescent formation and halts established anti-GBM glomerulonephritis in the rat. Lab.Invest. 89 470 PMID:19188913 |Zhang et al (2015) The c-Jun N-terminal kinase inhibitor SP600125 inhibits human cytomegalovirus replication. J.Med.Virol. 87 2135 PMID:26058558 |Vasilevskaya et al (2015) Inhibition of JNK sensitizes hypoxic colon cancer cells to DNA-damaging agents. Clin.Cancer.Res. 21 4143 PMID:26023085

Armepavine (R-Armepavine) exerted both in vitro and in vivo antifibrotic effects in rats, with inhibition of NF-κB, JunD and C EBP pathways. It improves experimental autoimmune crescentic glomerulonephritis.

Skimmin (Skimmine) has anti-inflammatory activity, can significantly improve renal function and suppress the IgG deposition as well as the development of glomerular lesions in a rat model of membranous glomerulonephritis.

Benzylthiouracil (6-Benzyl-2-thiouracil) induces ANCA-associated glomerulonephritis in Graves' disease patients and is used to study hyperthyroidism.

Sodium D-mannuronate, derived from the seaweed Macrocystis pyrifera, shows promise as a therapeutic agent in studies of autoimmune encephalomyelitis (EAE), adjuvant-induced arthritis (AIA), nephrotic syndrome, and acute glomerulonephritis [1].

NLRP3-IN-25 (compound 32), an orally available NLRP3 inhibitor, exhibits anti-inflammatory properties by attenuating renal injury in a mouse model of doxorubicin-induced glomerulonephritis and inhibiting IL-1β secretion in THP-1 cells, with an IC 50 value of 21 nM [1].