A VCP modulator; inhibits VCP ATPase activity (IC50 = 330 nM); inhibits tunicamycin-induced cell death

KUS121 – 1 mg

Brand:
Cayman
CAS:
1357164-52-3
Storage:
-20
UN-No:
Non-Hazardous - /

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}  

 

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Description

A VCP modulator; inhibits VCP ATPase activity (IC50 = 330 nM); inhibits tunicamycin-induced cell death, ATP depletion, and upregulation of CHOP in HeLa cells at 20, 50, and 50 μM, respectively; inhibits OGD-induced ATP depletion and cell death in rat primary cortical neurons in an in vitro model of cerebral ischemia at 100 μM; reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal MCAO at 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion; inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa at 50 mg/kg

Formal name: 4-amino-3-[2-[6-(4-fluoro-2-methylphenyl)-3-pyridinyl]diazenyl]-1-naphthalenesulfonic acid, monosodium salt

Synonyms: 

Molecular weight: 458.4

CAS: 1357164-52-3

Purity: ≥98%

Formulation: A crystalline solid

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