质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(C1=CC=CC=C1)/C=C\NC2=CC=CC([N+]([O-])=O)=C2
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-
InChI key
OVTJWWUGQKIRCL-KTKRTIGZSA-N
生化/生理作用
DJ001 is a selective, allosteric and non-competitive receptor protein tyrosine phosphatase-sigma (PTPσ) inhibitor (IC50 = 1.43 μM; >10 μM/20 other phosphatases) that promotes BM hematopoietic stem/progenitor cells (HSPCs) expansion (0.1-1 μg/mL or 0.373-3.73 μM; murine CD34- KSL cells) and suppresses radiation-induced BM HSC apoptosis (1-5 μg/mL; murine KSL & human CD34+ cells) via RhoGTPase/RAC1 activation and BCL-XL induction. DJ001 accelerates hematologic recovery and improves survival of irradiated mice in vivo (5 mg/kg/d s.c.). The (Z)- & (E)-isomers exist in equilibrium in polar solvents with (Z) showing enhanced binding-affinity to PTPσ catalytic & allosteric sites.
Selective, allosteric receptor protein tyrosine phosphatase-sigma (PTPσ) inhibitor that promotes BM hematopoietic stem/progenitor cells (HSPCs) expansion in vitro & in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Yurun Zhang et al.
Nature communications, 10(1), 3667-3667 (2019-08-16)
Receptor type protein tyrosine phosphatase-sigma (PTPσ) is primarily expressed by adult neurons and regulates neural regeneration. We recently discovered that PTPσ is also expressed by hematopoietic stem cells (HSCs). Here, we describe small molecule inhibitors of PTPσ that promote HSC regeneration
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