Chemical Structure : SCP1 inhibitor GR-28
CAS No.:
SCP1 inhibitor GR-28
(GR-28)
Catalog No.: PC-22168Not For Human Use, Lab Use Only.
SCP1 inhibitor GR-28 is a covalent small molecule inhibitor of small C-terminal domain phosphatase 1 (SCP1) with kinact/KI 1383 min-1 M-1, causes degrades REST protein in REST-dependent glioblastoma cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SCP1 inhibitor GR-28 is a covalent small molecule inhibitor of small C-terminal domain phosphatase 1 (SCP1) with kinact/KI 1383 min-1 M-1, causes degrades REST protein in REST-dependent glioblastoma cells.
GR-28 inhibits SCP1 capacity to dephosphorylate REST leading to accumulation of phospho-REST and its subsequent proteasomal degradation in vitro.
SCP1 inhibitor GR-28 covalently targets SCP1 Cys 181, and SCP1 C181A mutant shows resistance to GR-28 inhibition.
SCP1 inhibitor GR-28 (4 uM) reduces the transcriptional activity of REST and GR-28 (10 uM) is cytotoxic against high-REST GBM cells.
SCP1 inhibitor GR-28 exhibits profound synergy with ACSL inhibitor Triacsin C in high-REST GBM cells.
Physicochemical Properties
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M.Wt
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476.55
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Formula
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C26H24N2O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(3-(2'-methoxy-[1,1'-biphenyl]-4-carboxamido)propyl)cinnamamide 1,1-dioxide
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References
1. Svetlana B Panina, et al. BMC Biol. 2024 Apr 12;22(1):83.
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