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Biochem/physiol Actions
Brain-penetrant and selective cyclin-dependent kinase Cdk5/p25 complex inhibitor that improves neurodegenerative phenotypes in cultures and in vivo.
Cdk5i-FT is a brain-penetrant and selective cyclin-dependent kinase Cdk5/p25 complex inhibitor that is composed of Cdk5i, a human Cdk5-derived 12-aa p25-binding sequence (Kd = 220 nM) followed by a C-terminal TAT sequence and FITC-conjugated via a 6-aminohexanoate linker at its N-terminus. Cdk5i-FT inhibits Cdk5/p25 kinase activity in vitro by disrupting Cdk5-p25 interaction and protects neurons from Cdk5 hyperactivity-induced death in cultures (10 nM). Cdk5i-FT exhibits therapeutic efficacy in murine neurodegeneration models in vivo (20 mg/kg q.a.d. i.p.), using CK-p25 mice (with inducible p25 overexpress in forebrain neurons) and Tau P301S mice (with Cdk5-mediated Tau S301 hyperphosphorylation).
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Hygroscopic
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | (Powder or Lyophilized powder or film) |
| storage condition | desiccated |
| color | white to beige |
| storage temp. | -10 to -25°C |
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