DJ001 (C09-1126-589)

DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC 50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regenerationIn VitroDJ001 (5-1000 ng/mL; 3-7 days; BM KSL cells) treatment increases the percentages and numbers of BM KSL cells in culture compared with control cultures. DJ001 treatment also significantly increases the numbers of colony forming cells (CFCs) in 3 day culture of BM KSL cells. The BM KSL cells are irradiated with 300 cGy and placed in media (containing 20 ng/mL Thrombopoietin, 100 ng/mL stem cell factor (SCF), 50 ng/mL Flt3 ligand, TSF) with and without 1 μg/mL DJ001 for 3 days. DJ001 treatment increases recovery of BM CFCs and multipotent colony-forming unit–granulocyte erythroid monocyte megakaryocyte (CFU-GEMM) colonies compared with control cultures. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: BM KSL cells Concentration: 5 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL Incubation Time: 3 days or 7 days Result: Increased the percentages and numbers of BM KSL cells. Also significantly increased the numbers of colony forming cells (CFCs) in 3 day culture of BM KSL cells.In VivoDJ001 (5 mg/kg; subcutaneous injection; for 24 hours; female C57BL/6 mice) significantly decreases the percentage of apoptotic BM KSL cells in C57BL/6 mice at 24 h following 500 cGy TBI. DJ001 suppresses radiation-induced HSC apoptosis via activation of the RhoGTPase, RAC1, and induction of BCL-X L . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57BL/6 mice (8-10-week-old) irradiated with total body irradiation (TBI) Dosage: 5 mg/kg Administration: Subcutaneous injection; for 24 hours Result: Significantly decreased the percentage of apoptotic BM KSL cells in C57BL/6 mice at 24 h following 500 cGy TBI.Form:SolidIC50& Target:IC50: 1.43 μM (Protein tyrosine phosphatase-σ). Specification: 0.99 Molecular Formula: C15H12N2O3 Molecular Weight: 268.27 PubChem CID: 44161060 Isomeric SMILES: C1=CC=C(C=C1)C(=O)/C=C/NC2=CC(=CC=C2)[N+](=O)[O-]