DAPT

外観

白色～わずかにうすい黄色、結晶性粉末～粉末又は塊

溶解性

DMSO(10mg/mL)、メタノール(5mg/mL)ジメチルスルホキシドに溶ける。

使用上の注意

不活性ガス封入

使用

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells

生物活性

Inhibitor of γ -secretase; causes a reduction in A β 40 and A β 42 levels in human primary neuronal cultures (IC 50 values are 115 and 200 nM for total A β and A β 42 respectively) and in brain extract, cerebrospinal fluid and plasma in vivo . Does not effect APP α and APP β levels. Blocks Notch signaling in hybrid human-mouse foetal thymus organ culture (FTOC). Activity causes neural cells to commit to neuronal differentiation.

Biochem/physiol Actions

DAPT is a γ-secretase inhibitor and indirectly an inhibitor of Notch, a γ-secretase substrate. Other γ-secretase substrates include LDL receptor-related protein, E-cadherin and ErbB-4. As an inhibitor of γ-secretase, DAPT may be useful in the study of β-amyloid (Aβ) formation. DAPT has been shown to inhibit Notch signaling in studies of autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE), as well as in cancer cell growth, angiogenesis, and differentiation of human induced pluripotent stem cells (hIPSC).