Raphin1 acetate

CAS号

2242616-04-0

分子式

C10H12Cl2N4O2

主要靶点

Phosphatase

仅限科研使用

Cat No : CM05894

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Synonyms

inhibit|Inhibitor|Raphin 1|Raphin1|Raphin1 acetate|Raphin1 Acetate|Raphin-1 acetate|Raphin-1|phosphatase?PPP1R15B (R15B)|Phosphatase



产品信息

CAS号 2242616-04-0
分子式 C10H12Cl2N4O2
主要靶点 Phosphatase
主要通路 代谢
分子量 291.13
纯度 99.95%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|Inhibitor|Raphin 1|Raphin1|Raphin1 acetate|Raphin1 Acetate|Raphin-1 acetate|Raphin-1|phosphatase?PPP1R15B (R15B)|Phosphatase

靶点活性

R15B-PP1c holophosphatase:33 nM(Kd)

体内活性

Raphin1 具有口服生物利用度,能穿透血脑屏障,并在亨廷顿病的小鼠模型中展现了疗效。

体外活性

Raphin1是一种选择性抑制剂,针对R15B。在细胞中,Raphin1能迅速而短暂地增加其磷酸化底物的积累,导致蛋白质合成短暂减弱。在体外实验中,Raphin1通过干扰底物招募,抑制重组的R15B-PP1c整合酶活性,但不影响与之密切相关的R15A-PP1c。

溶解度

DMSO:40 mg/mL (137.4 mM)

参考文献

1.Krzyzosiak A, et al. Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B. Cell. 2018 Aug 23;174(5):1216-1228.e19.

The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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