Raphin1 acetate

Chemical Structure : Raphin1 acetate

CAS No.: 2242616-04-0

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货号: PC-21976Not For Human Use, Lab Use Only.

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25 mg	￥2180	In stock
50 mg	￥3780	In stock
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生物&药学活性

Raphin1 acetate (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	291.13
分子式	C10H12Cl2N4O2
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 acetate

参考文献

1. Krzyzosiak A, et al. Cell. 2018 Aug 23;174(5):1216-1228.e19.

Raphin1 acetate

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物理化学性质&存储条件

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Raphin1 acetate

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