MRK003
Product Specifications
CAS Number
623165-93-5
Target
Others, Apoptosis, Gamma-secretase
Related Pathways
Neuroscience, Others, Stem Cells, Proteases/Proteasome, Apoptosis
Bioactivity
MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway.
Smiles
C(C(F)(F)F)N1C[C@@]2([C@]3(CC=4C(C[C@@]2(CC3)[H])=CC=C(/C=C/CN5CCC(C(F)(F)F)CC5)C4)[H])NS1(=O)=O
Molecular Formula
C25H31F6N3O2S
Molecular Weight
551.59
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
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