Chemical Structure : Z218484536
CAS No.:
1223877-07-3
Z218484536
Catalog No.: PC-24886Not For Human Use, Lab Use Only.
Z218484536 is a potent and specific phosphoserine phosphatase (PSPH) inhibitor, inhibits the release of L-serine from cultured astrocytes with IC50 of 0.4 uM, reduces cellular L-serine levels with IC50 of 0.38 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Z218484536 is a potent and specific phosphoserine phosphatase (PSPH) inhibitor, inhibits the release of L-serine from cultured astrocytes with IC50 of 0.4 uM, reduces cellular L-serine levels with IC50 of 0.38 uM.
Z218484536 is highly selective against a panel of 20 protein tyrosine phosphatases, with only a weak inhibitory effect on DUSP22 at 30 uM.
Z218484536 has binding affinity for the A51V;G110A PSPH mutant (PSPH-MT) (6.1 uM), 26-fold lower than that for WT PSPH.
Z218484536 (2 mg/kg, i.p.) significantly reduced hippocampal levels of l-serine and d-serine in KA-induced chronic TLE mouse model.
Z218484536 (4 mg/kg) exhibited antiseizure effects in the KA mouse model of chronic temporal lobe epilepsy (TLE), also effectively reduced epileptic activity in the cynomolgus monkey TLE model.
Physicochemical Properties
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M.Wt
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247.23
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Formula
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C11H10FN5O
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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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(E)-2-((3-(4-fluorophenyl)-1H-pyrazol-4-yl)methylene)hydrazine-1-carboxamide
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References
1. Sha L, et al. Nat Chem Biol. 2025 Jun 2. doi: 10.1038/s41589-025-01920-5.
2. Patent CN119367357 A 2025-01-28.
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