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。
产品描述
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with IC50 of 1.43 μM. DJ001 promotes the regeneration of hematopoietic stem cells.
体外活性
Compared with control culture, DJ001 (5-1000 ng/mL; 3-7 days; BM KSL cells) treatment can increase the percentage and number of BM KSL cells in culture. DJ001 treatment also significantly increased the number of colony forming cells (CFC) in BM KSL cells cultured for 3 days. The BM KSL cells were irradiated with 300 cGy and placed in a medium containing 1 μg/mL DJ001 and without 1 μg/mL DJ001 (containing 20 μng/mL thrombopoietin, 100 μng/mL stem cell factor (SCF), 50 μng/mL Flt3 Body, TSF). 3 days. Compared with control culture, DJ001 treatment can improve the recovery rate of BM CFC and multipotent colony forming unit-granulocyte-like erythrocyte mononuclear megakaryocyte (CFU-GEMM) colonies[1].
体内活性
DJ001 inhibits radiation-induced HSC apoptosis by activating RhoGTPase, RAC1 and inducing BCL-XL. DJ001 (5 μg/kg; subcutaneous injection; duration 24 hours; female C57BL/6 mice) significantly reduced the percentage of apoptotic BM KSL cells in C57BL/6 mice 24h after 500°cGy TBI[1].
Cas No.
2161305-12-8
分子式
C15H12N2O3
分子量
268.27
储存和溶解度
DMSO:225mg/mL (838.7mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years