DJ001 (DJ-001, UCLA 5483071) is a highly selective, allosteric protein tyrosine phosphatase-sigma (PTPσ) inhibitor with IC50 of 1.5 uM.
DJ001 displays no inhibitory activity against 20 other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5.
DJ001 antagonizes PTPσ via unique non-competitive, allosteric binding.
DJ001 suppresses radiation-induced hematopoietic stem cells (HSCs) apoptosis via activation of the RhoGTPase, RAC1, and induction of BCL-XL.
DJ001 promoteds HSC regeneration, accelerates hematologic recovery, and improves survival in irradiated mice.
