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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-Raphin1
Raphin1

Chemical Structure : Raphin1

CAS No.: 2022961-17-5

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Raphin1 (PPP1R15B inhibitor Raphin1)

货号: PC-35503Not For Human Use, Lab Use Only.

Raphin1 (PPP1R15B inhibitor Raphin1) is a potent, selective, BBB-penetrant, orally bioavailable inhibitor of regulatory subunit of protein phosphatase 1, PPP1R15B, binds to the R15B-PP1c holophosphatase with Kd of 33 nM, 30-fold selective in binding R15B-PP1c over R15A-PP1c and did not bind to PP1c.

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10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3780 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Raphin1 (PPP1R15B inhibitor Raphin1) is a potent, selective, BBB-penetrant, orally bioavailable inhibitor of regulatory subunit of protein phosphatase 1, PPP1R15B, binds to the R15B-PP1c holophosphatase with Kd of 33 nM, 30-fold selective in binding R15B-PP1c over R15A-PP1c and does not bind to PP1c.
Raphin1 at 10 uM selectively inhibits R15B, but not R15A, in cells in the holophosphatase SPR assay, inducing a transient increase of eIF2a phosphorylation and attenuation of protein synthesis.
Raphin1 inhibits dephosphorylation of eIF2a by R15B-PP1c, but not by R15APP1c, promotes proteasome- and p97-dependent degradation of R15B.
Raphin1 demonstrates efficacy in a mouse model of Huntington’s disease in vivo.

物理化学性质&存储条件

分子量 231.08
分子式 C8H8Cl2N4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(E)-2-(2,3-dichlorobenzylidene)hydrazine-1-carboximidamide

参考文献

1. Agnieszka Krzyzosiak, et al. Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B. Cell. July 26, 2018DOI:https://doi.org/10.1016/j.cell.2018.06.030.

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