Biochem/physiol Actions

DJ001 is a selective, allosteric and non-competitive receptor protein tyrosine phosphatase-sigma (PTPσ) inhibitor (IC₅₀ = 1.43 µM; >10 µM/20 other phosphatases) that promotes BM hematopoietic stem/progenitor cells (HSPCs) expansion (0.1-1 µg/mL or 0.373-3.73 µM; murine CD34- KSL cells) and suppresses radiation-induced BM HSC apoptosis (1-5 µg/mL; murine KSL & human CD34+ cells) via RhoGTPase/RAC1 activation and BCL-XL induction. DJ001 accelerates hematologic recovery and improves survival of irradiated mice in vivo (5 mg/kg/d s.c.). The (Z)- & (E)-isomers exist in equilibrium in polar solvents with (Z) showing enhanced binding-affinity to PTPσ catalytic & allosteric sites.