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2161305-12-8

2161305-12-8 structure
2161305-12-8 structure
  • Name: DJ001
  • Chemical Name: DJ001
  • CAS Number: 2161305-12-8
  • Molecular Formula: C15H12N2O3
  • Molecular Weight: 268.27
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
  • Create Date: 2020-01-23 09:33:51
  • Modify Date: 2024-01-11 00:15:27
  • DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 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 regeneration[1].

Name DJ001
Description DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 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 regeneration[1].
Related Catalog
Target

IC50: 1.43 μM (Protein tyrosine phosphatase-σ)[1]

In Vitro DJ001 (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[1]. 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[1]. Cell Viability Assay[1] Cell 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 Vivo DJ001 (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-XL[1]. Animal Model: Female C57BL/6 mice (8-10-week-old) irradiated with total body irradiation (TBI)[1] 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.
References

[1]. Zhang Y, et al. PTPσ inhibitors promote hematopoietic stem cell regeneration. Nat Commun. 2019 Aug 14;10(1):3667.

Molecular Formula C15H12N2O3
Molecular Weight 268.27
Hazard Codes Xi