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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)
Biological Activity for Raphin 1
Raphin 1 is an 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.
Compound Libraries for Raphin 1
Raphin 1 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Raphin 1
| 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 for Raphin 1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.11 | 100 | |
| ethanol | 11.55 | 50 |
Preparing Stock Solutions for Raphin 1
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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Product Datasheets for Raphin 1
References for Raphin 1
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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Keywords: Raphin 1, Raphin 1 supplier, Raphin1, protein, phosphatase, 1, regulatory, subunit, 15B, inhibitors, inhibits, synthesis, PPP1R15B, huntingtin, Protein, Ser/Thr, Phosphatases, 6760, Tocris Bioscience
Citations for Raphin 1
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