DJ001

生物活性靶点体外研究体内研究 DJ001 试剂级价格

DJ001

CAS号:2161305-12-8
英文名:DJ001
中文名:DJ001
CBNumber:CB25848933
分子式:C15H12N2O3
分子量:268.27
MOL File:2161305-12-8.mol

DJ001化学性质

沸点 :417.7±45.0 °C(Predicted)
密度 :1.297±0.06 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml with warming)
形态 :solid
酸度系数(pKa) :-1.30±0.70(Predicted)
颜色 :Yellow
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

DJ001性质、用途与生产工艺

生物活性 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。
靶点

IC50: 1.43 μM (Protein tyrosine phosphatase-σ)

体外研究

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.

体内研究

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-X _L .

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.