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.
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
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Not applicable
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Not applicable
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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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