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Raphin1 acetate
- Parent CAS: 2022961-17-5
- Soluble in DMSO
- MF: C8H8Cl2N4.C2H4O2
- MW: 291.13
Description
Raphin1 acetate is a selective inhibitor of PPP1R15B (R15B) and bound strongly (Kd value of 0.033 μM) to the R15B-PP1c holophosphatase. Moreover, Raphin1 acetate was ~30-fold selective in binding R15B-PP1c over R15A-PP1c and did not bind to PP1c. In cells, Raphin1 acetate caused a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis. In vitro, Raphin1 acetate inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment. Raphin1 acetate was orally bioavailable, crossed the blood-brain barrier, and demonstrated efficacy in a mouse model of Huntington’s disease. This product is also available as the free base (Axon 3004)
More Information
| Parent CAS No. | 2022961-17-5 |
|---|---|
| Chemical Name | (E)-2-(2,3-Dichlorobenzylidene)hydrazinecarboximidamide acetate |
| SMILES | C1(Cl)C(Cl)=C(/C=N/NC(N)=N)C=CC=1.CC(=O)O |
| MFCD | N.A. |
| InChi | InChI=1S/C8H8Cl2N4.C2H4O2/c9-6-3-1-2-5(7(6)10)4-13-14-8(11)12;1-2(3)4/h1-4H,(H4,11,12,14);1H3,(H,3,4)/b13-4+; |
| InChiKey | WSDLUFBVKWLRSN-GAYQJXMFSA-N |
| CID | 139035044 |
| Short Description | PPP1R15B (R15B) inhibitor |
