1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. DJ001

DJ001 

Cat. No.: HY-133146
Handling Instructions

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.

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DJ001 Chemical Structure

DJ001 Chemical Structure

CAS No. : 2161305-12-8

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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].

IC50 & 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.
Molecular Weight

268.27

Formula

C₁₅H₁₂N₂O₃

CAS No.

2161305-12-8

SMILES

O=C(C1=CC=CC=C1)/C=C\NC2=CC=CC([N+]([O-])=O)=C2

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DJ001DJ 001DJ-001PhosphatasePTPσhematopoieticregenerationapoptosisnumbersHSCRhoGTPaseRAC1BCL-XLInhibitorinhibitorinhibit

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