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Chemical Structure : Raphin1 acetate
CAS No.: 2242616-04-0
Catalog No.: PC-21976Not For Human Use, Lab Use Only.
Raphin1 acetate (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.
| 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 acetate (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 | 291.13 | |
| Formula | C10H12Cl2N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
(E)-2-(2,3-dichlorobenzylidene)hydrazine-1-carboximidamide acetate |
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1. Krzyzosiak A, et al. Cell. 2018 Aug 23;174(5):1216-1228.e19.
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