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.

Product information

CAS Number: 2161305-12-8

Molecular Weight: 268.27

Formula: C15H12N2O3

Chemical Name: (Z)-3-(3-nitroanilino)-1-phenylprop-2-en-1-one

Smiles: [O-][N+](=O)C1=CC(=CC=C1)NC=CC(=O)C1C=CC=CC=1

InChiKey: OVTJWWUGQKIRCL-MDZDMXLPSA-N

InChi: InChI=1S/C15H12N2O3/c18-15(12-5-2-1-3-6-12)9-10-16-13-7-4-8-14(11-13)17(19)20/h1-11,16H/b10-9+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (931.90 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.

References:

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

Products are for research use only. Not for human use.