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DJ001 Sale

目录号 : GC39295

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。

DJ001 Chemical Structure

Cas No.:2161305-12-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,465.00
现货
5mg
¥3,150.00
现货
10mg
¥4,950.00
现货
50mg
¥14,850.00
现货
100mg
¥20,250.00
现货
200mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration[1].

[1]. Zhang Y, et al. PTPσ inhibitors promote hematopoietic stem cell regeneration. Nat Commun. 2019 Aug 14;10(1):3667.

Chemical Properties

Cas No. 2161305-12-8 SDF
Canonical SMILES O=C(C1=CC=CC=C1)/C=C\NC2=CC=CC([N+]([O-])=O)=C2
分子式 C15H12N2O3 分子量 268.27
溶解度 DMSO: 250 mg/mL (931.90 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.7276 mL 18.6379 mL 37.2759 mL
5 mM 0.7455 mL 3.7276 mL 7.4552 mL
10 mM 0.3728 mL 1.8638 mL 3.7276 mL
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Research Update

PTPσ inhibitors promote hematopoietic stem cell regeneration

Nat Commun 2019 Aug 14;10(1):3667.PMID:31413255DOI:PMC6694155

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 in vivo. Systemic administration of the PTPσ inhibitor, DJ001, or its analog, to irradiated mice promotes HSC regeneration, accelerates hematologic recovery, and improves survival. Similarly, DJ001 administration accelerates hematologic recovery in mice treated with 5-fluorouracil chemotherapy. DJ001 displays high specificity for PTPσ and antagonizes PTPσ via unique non-competitive, allosteric binding. Mechanistically, DJ001 suppresses radiation-induced HSC apoptosis via activation of the RhoGTPase, RAC1, and induction of BCL-XL. Furthermore, treatment of irradiated human HSCs with DJ001 promotes the regeneration of human HSCs capable of multilineage in vivo repopulation. These studies demonstrate the therapeutic potential of selective, small-molecule PTPσ inhibitors for human hematopoietic regeneration.