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DAPT(GSI-IX)
Cat No.
CEI-0206
Description
DAPT can inhibit gamma-secretase with IC50 of 20 nM.
Alias
GSI-IX
CAS No.
208255-80-5
Molecular Weight
432.464
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
GSI-IX
Targets
gamma-secretase
Molecular Formula
C23H26F2N2O4
Chemical Name
(S)-tert-butyl 2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate
Solubility
DMSO 87 mg/mL Water
In vitro
DAPT, (N-{N-[2-(3,5-Difluorophenyl)acetyl]-(S)-alanyl}-(S)-phenylglycine tert-butyl ester), is a inhibitor of gamma-secretase( IC50=20 nM), which is involved in Alzheimers disease. DAPT also can inhibit cdk5. Its interesting that DAPT attenuated activity of CDK5, but DAPT can up-regulate the level of CDK5. DAPT can disrupt cdk5 and p35 interaction. DAPT up-regulated neurogenin that is negatively regulated by Notch, and down-regulated Hes1, a downstream target of Notch.
In vivo
Neurons treated with 10 microM DAPT showed attenuated cdk5 activity in spite of an up-regulation of cdk5 protein level, consistent with a phenomenon reported in the cdk5 transgenic mice. In U87MG xenograft mouse models, DAPT treatment increased tumor vessel density but compromised vessel function, as evidenced by poor perfusion and aggravated hypoxia.
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