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5-(3-(4-氟苯基)-1-苯基-1H-吡唑-4-基)咪唑啉-2,4-二酮

用途

DPH 是一种有效的,细胞渗透的 c-Abl 激活剂,在酶和细胞活动中,能够有效刺激 c-Abl 的活化。

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名称

[ CAS 号 ]:
484049-04-9

[ 中文名 ]:
5-(3-(4-氟苯基)-1-苯基-1H-吡唑-4-基)咪唑啉-2,4-二酮

[ 英文名 ]:
DPH

[英文别名 ]:

HMS2301N21
DPH

生物活性

[ 描述 ]:

DPH 是一种有效的,细胞渗透的 c-Abl 激活剂,在酶和细胞活动中,能够有效刺激 c-Abl 的活化。

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> BCR-ABL

研究领域 >> 癌症

[体外研究]

DPH与肉豆蔻酰结合位点结合并通过空间位阻阻止αI螺旋的弯曲构象的形成,这种作用方式不同于先前鉴定的变构c-Abl抑制剂GNF-2,其也与肉豆蔻酰结合位点结合。。 DPH代表第一种用于c-Abl活化的细胞渗透性小分子工具化合物[1]。

[参考文献]

[1]. Yang J, et al. Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site. Chem Biol. 2011 Feb 25;18(2):177-86

[2]. Shapiro LP, et al. Corticosteroid-induced dendrite loss and behavioral deficiencies can be blocked by activation of Abl2/Arg kinase. Mol Cell Neurosci. 2017 Oct 26;85:226-234.

[相关活性小分子]

物理化学性质

[ 分子式 ]:
C₁₈H₁₃FN₄O₂

[ 分子量 ]:
336.32000

[ 精确质量 ]:
336.10200

[ PSA ]:
83.00000

[ LogP ]:
2.47480

[ 储存条件 ]:
2-8℃

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

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