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YO-01027

CAS No. : 209984-56-5

MCE 站：YO-01027

产品活性：YO-01027 (Dibenzazepine; DBZ) 是高效的 γ-分泌酶抑制剂，裂解 Notch 和 APPL 的 IC₅₀ 分别为 2.92 和 2.64 nM。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：Notch  |  γ-secretase

In Vitro: Increasing concentrations of 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. The molecular targets of CE and DBZ are the N-terminal fragment of presenilin 1 within the γ-secretase complex.

In Vivo: DBZ blocks activated Notch1 signaling in abdominal aortic aneurysm (AAA) tissue from both Ang II-infused Apo E^-/- mice and human undergoing AAA repair. DBZ markedly prevents Ang II-stimulated accumulation of macrophages and CD4+ T cells, and ERK-mediated angiogenesis, simultaneously reverses Th2 response, in vivo. Administration of DBZ markedly attenuates renal fibrosis and expression of fibrotic markers, including collagen 1α1/3α1, fibronectin, and α-smoothmuscle actin. DBZ significantly inhibits ureteral obstruction -induced expression of transforming growth factor (TGF)- β, phosphorylated Smad 2, and Smad 3.

相关产品：Bioactive Compound Library Plus  |  Neuronal Signaling Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  DAPT  |  Valproic acid  |  LY-411575  |  Compound E  |  CB-103  |  Tangeretin  |  Jagged-1 (188-204) (TFA)  |  E 2012  |  IMR-1  |  L-685458  |  Semagacestat  |  Carvacrol  |  RBPJ Inhibitor-1  |  JI051  |  Bruceine D  |  NGP555  |  BMS 299897  |  ZLDI-8  |  Psoralidin  |  Sulindac sulfide  |  Begacestat  |  Z-Ile-Leu-aldehyde  |  gamma-secretase modulator 3  |  BMS 433796  |  SAHM1  |  tCFA15

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