A potent

Ro 4929097 – 5 mg

Brand:
Cayman
CAS:
847925-91-1
Storage:
-20
UN-No:
Non-Hazardous - /

Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}  

 

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Description

A potent, selective inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively); orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation

Formal name: N1-[(7S)-6,7-dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-pentafluoropropyl)-propanediamide

Synonyms: 

Molecular weight: 469.4

CAS: 847925-91-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Angiogenesis||Research Area|Cell Biology|Cell Signaling|Notch Signaling||Research Area|Cell Biology|Proteolysis|Lysosomal Proteases||Research Area|Neuroscience

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