YO-01027 (Dibenzazepine) (209984-56-5) Description:
Dibenzazepine, also known as YO-01027 and Iminostilbene, is a potent γ-secretase inhibitor. Dibenzazepine also potently blocks amyloid precursor protein-like (APPL) and Notch cleavage. γ-Secretase is a fascinating, multi-subunit, intramembrane cleaving protease that is now being considered as a therapeutic target for a number of diseases. Potent, orally bioavailable γ-secretase inhibitors (GSIs) have been developed and tested in humans with Alzheimer’s disease (AD) and cancer.
YO-01027 is a dipeptidic gamma-secretase inhibitor with IC50 of 2.6 and 2.9 nM for the proteolysis of APPL and Notch, respectively. YO-01027 is used as an anti-Alzheimer agent. YO-01027 directly interact with the gamma-secretase complex. Unlike other gamma-secretase inhibitors,YO-01027 targets different functional domain of the complex. YO-01027 targets the N-terminal Presenilin fragment as well as another gamma-secretase inhibitor Compound E (Cpn E), whereas DFK167 and DAPT, another two gamma-secretase inhibitors, bind to the catalytic site of the Presenilin aspartyl protease subunit and the C-terminal Presenilin fragment, respectively. In a study, YO-01027 and CpnE indicated no apparent discrimination in blocking APPL and Notch cleavages, displaying statistically equivalent IC50 values for both substrates.
YO-01027 (Dibenzazepine) (209984-56-5) Specifications:
|Synonyms||YO-01027; YO 01027; YO01027; Dibenzazepine; DBZ; Iminostilbene; Deshydroxy LY-411575.|
|Purity||>98% (or refer to the Certificate of Analysis)|
|Monoisotopic Mass||463.171 g/mol|
|SMILES||C[[email protected]](NC(CC1=CC(F)=CC(F)=C1)=O)C(N[[email protected]@H]2C(N(C)C3=CC=CC=C3C4=CC=CC=C24)=O)=O|
|Color||Yellow to orange|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||Inhibits γ-secretase and Notch signaling|