DJ001

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DJ001 是一种高度特异性，选择性和非竞争性的蛋白酪氨酸磷酸酶-σ (PTPσ) 抑制剂，IC50 为 1.43 μM。DJ001 对其他磷酸酶无抑制活性，对蛋白质磷酸酶 5 仅有中等抑制活性。DJ001 促进造血干细胞再生。

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.

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.Cell Viability Assay 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.

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.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.

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Metabolic Enzyme/Protease

Phosphatase

Phosphatase

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2161305-12-8

268.27

C15H12N2O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (931.90 mM; 超声助溶 )

N(/C=C\C(=O)C1=CC=CC=C1)C2=CC(N(=O)=O)=CC=C2

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(-20℃)

With Ice Pack

≥ 2 years