Raphin 1

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Cat.No. 6760 - Raphin 1 | C8H8Cl2N4 | CAS No. 2022961-17-5
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% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2022961-17-5
PubChem ID 5356739
InChI Key WLTSTDGGFCQWTK-PQMHYQBVSA-N
Smiles NC(N/N=C/C1=C(C(Cl)=CC=C1)Cl)=N

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.11 100
ethanol 11.55 50

Preparing Stock Solutions

The following data is based on the product molecular weight 231.08. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.33 mL 21.64 mL 43.28 mL
5 mM 0.87 mL 4.33 mL 8.66 mL
10 mM 0.43 mL 2.16 mL 4.33 mL
50 mM 0.09 mL 0.43 mL 0.87 mL

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References

References are publications that support the biological activity of the product.

Krzyzosiak et al (2018) Target-based discovery of an inhibitor of the regulatory phosphatase PPP1R15B. Cell. 174 1216 PMID: 30057111


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