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DAPT

產(chǎn)品活性：DAPT (GSI-IX) 是一種有效的，口服活性的 γ 分泌酶 (γ-secretase) 抑制劑，對(duì)總 amyloid-β (Aβ) 和 Aβ₄₂ 的 IC₅₀ 分別為 115 nM 和 200 nM。DAPT 抑制 Notch 1 信號(hào)傳導(dǎo)并誘導(dǎo)細(xì)胞分化。DAPT 還可誘導(dǎo)細(xì)胞自噬 (autophagy) 和凋亡 (apoptosis)。DAPT 具有神經(jīng)保護(hù)活性，并可用于自身免疫性和淋巴增生性疾病，退化性疾病和癌癥的研究。

研究領(lǐng)域：Neuronal Signaling  |  Stem Cell/Wnt  |  Autophagy  |  Apoptosis

作用靶點(diǎn)：γ-secretase  |  Amyloid-β  |  Autophagy  |  Notch  |  Apoptosis

In Vitro: DAPT inhibits Aβ production over 90%, effects only a modest reduction in APPβ in the culture media. Although APPβ is reduced by about 30% by DAPT treatment, this effect is not concentration-dependent and is reversed by the removal of DAPT.
CNE-2 cells are treated with increasing concentrations of DAPT (0, 25, 50 and 75 μM), and the γ-secretase-generated Notch 1 fragment Val1744-NICD is decreased after 48 h in a dose-dependent manner (P<0.01). The activation of γ-secretase is almost completely inhibited by DAPT at the concentration of 50 μM.

In Vivo: DAPT is administered to PDAPP mice (100 mg/kg s.c.) and the levels of DAPT and Aβ are examined in the brain cortex. Peak DAPT levels of 490 ng/g are achieved in the brain 3 h after treatment, and levels greater than 100 ng/g (~200 nM) are sustained throughout the first 18 h. These brain concentrations of DAPT are in excess of its IC₅₀ for lowering Aβ in neuronal cultures (115 nM), and results in a robust and sustains pharmacodynamic effect.
DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and Nuclear factor kappa B in rats. Western blot analyses also show a significant decrease of Notch 1 and NF-κB expression in DAPT (0.03 mg/kg) group (P<0.05 vs. MCAO group).

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Immunology/Inflammation Compound Library  |  Neuronal Signaling Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Peptidomimetic Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  Anti-Alzheimer's Disease Compound Library  |  Neuroprotective Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Angiogenesis-Related Compound Library  |  Transcription Factor-Targeted Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Cancer Stem Cells Compound Library  |  Membrane Protein-targeted Compound Library  |  SY-5609  |  BRD4 Inhibitor-18  |  THK-523  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  AAPK-25  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  Abacavir sulfate  |  Meloxicam-d₃-1  |  Thailanstatin D  |  SB-218078  |  Toyocamycin  |  Sorafenib-d₄  |  Busulfan  |  PTC-028  |  Dinaciclib  |  β-Amyloid (12-28)  |  CR-1-31-B  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  AZA1  |  Bleomycin A5  |  NIAD-4  |  Xevinapant  |  Mangiferin  |  Cambinol

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