CHZ868 is an inhibitor of type II JAK2 with an IC50 value of 0.17 μM in EPOR JAK2 WT Ba/F3 cells. CHZ868 demonstrates 60- to 70-fold higher inhibition of JAK1-/TYK2-mediated nuclear STAT1 translocation compared to pan-JAK inhibitors.

Tin Protoporphyrin IX dichloride (NSC 267099, SnPPIX, Sn-Protoporphyrin) is a potent inhibitor of heme oxygenase-1 (HO-1), reduces ozone-induced pulmonary inflammation and BAL cell necrosis, highlighting its protective role. It also sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in a mouse model, suggesting its potential for PDAC treatment.

Fumonisin B1 (Macrofusine) is a mycotoxin produced by Fusarium moniliforme Sheldon and a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase), an enzyme vital for the de novo synthesis of sphingolipids. It exhibits an IC50 of 0.1 µM for N-acyltransferase (ceramide synthase) in rat liver microsomes and also reduces the conversion of [3H]sphingosine to [3H]ceramide in […]

GSK199 is a reversible, specific inhibitor of peptidyl arginine deiminase 4 (PAD4), with an IC50 of 200 nM without calcium. It is involved in histone citrullination and neutrophil extracellular trap formation, making it useful for studying autoimmune, cardiovascular, and oncological diseases.

Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.

Lestaurtinib (CEP-701, KT-5555) is a derivative of the indolocarbazole K252 and a staurosporine analog. It is an orally active inhibitor of receptor protein tyrosine kinases (RPTKs), which inhibits FLT3 and Trk, with an IC50 of 3 nM and < 25 nM, respectively. It also inhibits JAK2 with an IC50 of 0.9 nM.