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Chemical Structure| 209984-56-5 Chemical Structure| 209984-56-5
Chemical Structure| 209984-56-5

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CAS No.: 209984-56-5

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Dibenzazepine is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.

Synonyms: DBZ; Dibenzazepine; Deshydroxy LY-411575.

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Product Details of YO-01027

CAS No. :209984-56-5
Formula : C26H23F2N3O3
M.W : 463.48
SMILES Code : C[C@H](NC(=O)CC1=CC(F)=CC(F)=C1)C(=O)N[C@H]1C2=CC=CC=C2C2=CC=CC=C2N(C)C1=O
Synonyms :
DBZ; Dibenzazepine; Deshydroxy LY-411575.
MDL No. :MFCD12828734
InChI Key :QSHGISMANBKLQL-OWJWWREXSA-N
Pubchem ID :11454028

Safety of YO-01027

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Enteroids 5 mM 10 days To examine the impact of YO-01027 on enteroid formation and self-renewal. PMC9133587
B16F10 melanoma cells 25 μg/ml and 50 μg/ml 24 h The cytotoxic effect of combined therapies was evaluated, showing significant reduction in cell viability and increased apoptosis. PMC7237551
colon normal organoids 2.5 μM 48 hours To investigate the effect of Notch signaling blockade on the differentiation of colon normal organoids, results showed that DBZ promoted the differentiation of secretory goblet cells. PMC11058856
colon tumor organoids 5 μM 72 hours To investigate the effect of Notch signaling blockade on the differentiation of colon tumor organoids, results showed that DBZ failed to induce any mucosecretory gene expression. PMC11058856
K457 human melanoma cells 25 μg/ml 3 days Anti-Notch1 induced 75% cell death PMC11533310
YUMM1.7 mouse melanoma cells 25 μg/ml 3 days Anti-Notch1 induced 80% cell death PMC11533310
YUMM2.1 mouse melanoma cells 25 μg/ml 3 days Anti-Notch1 induced 55% cell death PMC11533310

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
C57BL/6 mice YUMM2.1 and YUMM1.7 mouse melanoma models Intraperitoneal injection 10 mg/kg every other day for 15 days Anti-Notch1 significantly delayed tumor growth and altered the TME, reducing immunosuppressive cells and increasing CD8+ T cells PMC11533310

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.58mL

4.32mL

2.16mL

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