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Enzymes for Research, Diagnostic and Industrial Use

RO4929097

Cat No.
CEI-0203
Description
RO4929097 can inhibit gamma-secretase with IC50 of 4 nM.
CAS No.
847925-91-1
Molecular Weight
469.4
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
Gamma-secretase
Molecular Formula
C22H20F5N3O3
Chemical Name
Propanediamide, N1-[(7S)-6,7-dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-pentafluoropropyl)-
Solubility
DMSO 94 mg/mL Water
In vitro
RO4929097 is a novel inhibitor of gamma secretase, which is a key component of the enzymatic complex that cleaves and activates NOTCH. In human primary melanoma cell lines, RO4929097 decreased the levels of NOTCH transcriptional target HES1. RO4929097 also reduced proliferation and impaired ability to form colonies in soft agar and to organize in tridimensional spheres.
In vivo
RO4929097 affected the growth of human primary melanoma xenograft in NOD/SCID/IL2gammaR-/- mice and inhibited subsequent tumor formation in a serial xenotransplantation model. Inhibition of NOTCH signaling suppresses the tumor initiating potential of melanoma cells. RO4929097 decreased tumor volume and blocked the invasive growth pattern of metastatic melanoma cell lines in vivo. But, for IL6 and IL8 overexpressing tumors, RO4929097 no longer impacts angiogenesis or the infiltration of tumor associated fibroblasts.
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