Raphin 1

Catalog # Availability Size / Price Qty
6760/10
6760/50
Protein Ser/Thr Phosphatase Inhibitors Small Molecule
1 Image
Description: Inhibitor of the regulatory subunit PPP1R15B of protein phosphatase 1; orally bioavailable and brain penetrant

Chemical Name: (2E)-2-[(2,3-Dichlorophenyl)methylene]hydrazinecarboximidamide

Purity: ≥98%

Product Details
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Biological Activity

Inhibitor of the regulatory subunit PPP1R15B of protein phosphatase (Kd = 33 nM). Displays >30-fold selectivity for PPP1R15B over PPP1R15A. Inhibits PPP1R15B-mediated dephosphorylation and protein synthesis in vitro. Induces transient reduction in protein synthesis in brains of wild type mice after single dose. Decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in a mouse model of Huntington's disease. Orally bioavailable and brain penetrant.

Technical Data

M.Wt:
231.08
Formula:
C8H8Cl2N4
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2022961-17-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Target-based discovery of an inhibitor of the regulatory phosphatase PPP1R15B.
    Krzyzosiak et al.
    Cell., 2018;174:1216

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