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2161305-12-8

中文名稱 DJ001
英文名稱 DJ001
CAS 2161305-12-8
分子式 C15H12N2O3
分子量 268.27
MOL 文件 2161305-12-8.mol
更新日期 2023/03/20 15:41:25
2161305-12-8 結(jié)構(gòu)式 2161305-12-8 結(jié)構(gòu)式

基本信息

中文別名
化合物DJ001
化合物 T11053
英文別名
DJ001

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C
溶解度溶于 DMSO(最高 50 mg/ml)或乙醇(升溫最高 10 mg/ml)
形態(tài)固體
顏色黃色
穩(wěn)定性可在-20°C下的DMSO或乙醇溶液保存長達(dá)3個(gè)月。

常見問題列表

生物活性
DJ001 是一種高度特異性,選擇性和非競爭性的蛋白酪氨酸磷酸酶-σ (PTPσ) 抑制劑,IC50 為 1.43 μM。DJ001 對(duì)其他磷酸酶無抑制活性,對(duì)蛋白質(zhì)磷酸酶 5 僅有中等抑制活性。DJ001 促進(jìn)造血干細(xì)胞再生。
靶點(diǎn)

IC50: 1.43 μM (Protein tyrosine phosphatase-σ)

體外研究

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.
體內(nèi)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.
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