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Merck
CN

SML3955

Sigma-Aldrich

Cdk5i-FT trifluoroacetate

≥95% (HPLC)

Synonym(s):

Ahx = 6-aminohexanoate) trifluoroacetate, FITC-Ahx-ARAFGIPVRCYS-TAT trifluoroacetate, FITC-Ahx-ARAFGIPVRCYS-YGRKKRRQRRR (FITC = fluorescein isothiocyanate, FITC-Ahx-Cdk5i-TAT trifluoroacetate

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About This Item

Empirical Formula (Hill Notation):
C151H232N52O34S2 · xC2HF3O2
Molecular Weight:
3383.92 (free base basis)
UNSPSC Code:
12352200
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Quality Level

Assay

≥95% (HPLC)

form

(Powder or Lyophilized powder or film)

storage condition

desiccated

color

white to beige

storage temp.

-10 to -25°C

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).

Disclaimer

Hygroscopic

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Ping-Chieh Pao et al.
Proceedings of the National Academy of Sciences of the United States of America, 120(16), e2217864120-e2217864120 (2023-04-13)
Aberrant activity of cyclin-dependent kinase (Cdk5) has been implicated in various neurodegenerative diseases. This deleterious effect is mediated by pathological cleavage of the Cdk5 activator p35 into the truncated product p25, leading to prolonged Cdk5 activation and altered substrate specificity.

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