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Chemical Structure : Raphin1
CAS No.: 2022961-17-5
Catalog No.: PC-35503Not For Human Use, Lab Use Only.
Raphin1 (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 did not bind to PP1c.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $378 | In stock | |
| 100 mg | Get quote |
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Raphin1 (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.
| M.Wt | 231.08 | |
| Formula | C8H8Cl2N4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(E)-2-(2,3-dichlorobenzylidene)hydrazine-1-carboximidamide |
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1. Agnieszka Krzyzosiak, et al. Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B. Cell. July 26, 2018DOI:https://doi.org/10.1016/j.cell.2018.06.030.
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