Raphin1

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Raphin1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2022961-17-5

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

Raphin1 是一种口服生物可利用的，选择性调节性磷酸酶 PPP1R15B (R15B) 抑制剂。Raphin1 与 R15B-PP1c 全磷酸酶强烈结合 (Kd=33 nM)，与 R15A-PP1c 相比，结合 R15B-PP1c 约为其 30 倍的选择性。Raphin1 穿过血脑屏障，并减少蛋白质错误折叠疾病的小鼠模型中的生物和分子缺陷。

Cas No.	2022961-17-5
Canonical SMILES	N=C(N/N=C/C1=CC=CC(Cl)=C1Cl)N
分子式	C₈H₈Cl₂N₄
分子量	231.08
溶解度	DMSO: 125 mg/mL (540.94 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1]. Raphin1 causes a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis[1].Raphin1 inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment[1]. Raphin1 improves weight of HD82Q mice treated from 4 to ∼10 weeks of age with 2 mg/kg of Raphin1 once a day by oral gavage. Raphin1 also decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice[1]. [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.