PKC Activator VIII; CGK062

Code: 5042760001 D2-231

Biochem/physiol Actions

Reversible: yes

General description

A cell permeable coumarin-containing compound that is shown to activate PKCα act...


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Your Price
€229.82 EACH
€282.68 inc. VAT

Biochem/physiol Actions

Reversible: yes

General description

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.

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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Gwak, J., et al. 2012. PLoS One.7, e46697.

Packaging

Packaged under inert gas

2 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)

assay≥98% (HPLC)
coloroff-white
formsolid
manufacturer/tradenameCalbiochem®
potency12.2 µM IC50
Quality Level100
solubilityDMSO: 100 mg/mL
storage conditionprotect from light, OK to freeze
storage temp.−20°C
Cas Number1001129-59-4
This product has met the following criteria to qualify for the following awards:



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