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Description
Overview
A cell permeable coumarin-containing compound that is shown to activate PKCα activity and induce cellular PKCα membrane translocation (Effective conc. 12.5 to 50 µM) as well as PKCα-mediated signaling events. Effectively affects the viability of CRT-dependent cancer cells (IC50 = 1.62 to 18.6 µM; 48 h) in vitro and suppresses PC3-derived tumor expansion in mice (50 & 100 mg/kg/day; i.p) in vivo, while exhibiting little cytotoxicity toward WI38 normal fibroblasts.
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
14-June-2013 JSW
Synonyms
Protein Kinase C Activator VII
Description
A cell permeable coumarin-containing compound that is shown to activate PKCα activity toward GST-β-catenin or PKC substrate peptide in cell-free kinase assays (12.5 & 25 µM) and induce cellular PKCα membrane translocation (Effective conc. 12.5 to 50 µM in HEK293, PC3, SNU475, and SW480 cultures) as well as PKCα-mediated β-catenin phosphorylation (Ser33/37/45) and subsequent β-catenin degradation in a F-box Ub ligase complex component β-TrCP- (β-transducin repeat-containing protein) dependent, but GSK-3β-independent, manner. Effectively affects the viability of CRT- (β-catenin response transcription) dependent cancer cells (IC50 = 1.62, 5.71, 9.40, 11.41, and 18.60 µM, respectively, in SW480, HCT15, PC3, SNU475, and DLD-1 cultures; 48 h) in vitro and suppresses PC3-derived tumor expansion in mice (23% and 11% of control size, respectively, with 50 or 100 mg/kg daily i.p. dose for 4 wks) in vivo, while exhibiting little cytotoxicity toward WI38 normal fibroblasts (IC50 = 74.83 µM; 48 h).
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₃H₂₀O₇
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
-20°C
Protect from light
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.