YO-01027 (Dibenzazepine) (GMP) is YO-01027 synthesized following Good Manufacturing Practice (GMP) standards. GMP-compliant small molecules serve effectively as ancillary agents in the production of cell therapies. YO-01027 acts as a potent inhibitor of γ-secretase [1][2].
体内研究
DBZ inhibits activated Notch1 signaling in abdominal aortic aneurysm (AAA) tissue from both Ang II-infused Apo E-/- mice and humans undergoing AAA repair. DBZ significantly reduces Ang II-stimulated accumulation of macrophages and CD4+ T cells, inhibits ERK-mediated angiogenesis, and concurrently reverses Th2 response, in vivo[3].
Administration of DBZ significantly reduces renal fibrosis and the expression of fibrotic markers, such as collagen 1α1/3α1, fibronectin, and α-smooth muscle actin (α-SMA). DBZ effectively suppresses the expression of transforming growth factor (TGF)-β, phosphorylated Smad 2, and Smad 3 induced by ureteral obstruction [4].
体外研究
Elevating levels of DBZ administered to cells expressing APPL or Notch result in a gradual buildup of APPL CTF fragments and a reduction in NICD production, following a strictly dose-dependent pattern[1].
CE and DBZ target the N-terminal fragment of presenilin 1 within the γ-secretase complex[2].
YO-01027 (0.25-10 μM, during 1-18 days) enhances the generation of induced pluripotent stem cells (iPSCs) from human neonatal keratinocytes [2].
YO-01027 (at 2 μM for 3 days) does not alter p53 activity in human keratinocytes transduced with OCT4 and SOX2 [2].
YO-01027 (10 μM, 3 days) enhances the proliferation of supporting cells (SCs) in cultured mouse cochleae [3].
YO-01027 (10 μM, 3 days) induces the generation of new hair cells (HCs) and augments the total number of HCs in neonatal mouse cochleae [3].
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