Description
YO-01027 (Dibenzazepine, DBZ) can inhibit gamma-secretase with IC50 of 2.6 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C26H23F2N3O3
Chemical Name
7-(S)-[N(3,5-difluorophenylacetyl)-L-alaninyl]amino-5-methyl-5,7-dihydro-6H-dibenz[b,d]azepin-6-one
Solubility
DSMO 93 mg/mL Water
In vitro
YO-01027 (Dibenzazepine, DBZ) administered to APPL- or Notch-expressing cells leads to the progressive accumulation of APPL CTF fragments and a decrease in NICD production in a strictly dose-dependent manner.As a gamma-secretase inhibitor, YO-01027 (Dibenzazepine, DBZ) is more potent than CpnE, DAPT, and DFK167.YO-01027 (Dibenzazepine, DBZ) showed no apparent discrimination in blocking APPL and Notch cleavages.
In vivo
In vivo, YO-01027 (Dibenzazepine, DBZ) significantly decrease MCF7 but not MDA-MB-231 tumours and increase latency compared to control mice (18 to 28 days). YO-01027 (Dibenzazepine, DBZ)-treated MCF7 tumours that did form had significantly reduced tumour volumes.
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