Merck
  • 504276
All Photos(1)

5.04276

Sigma-Aldrich

PKC Activator VII, CGK062

All Photos(1)
Synonym(s):
PKC Activator VII, CGK062, Protein Kinase C Activator VII
Empirical Formula (Hill Notation):
C23H20O7
Molecular Weight:
408.40

アッセイ

≥98% (HPLC)

品質水準

100

形状

solid

有効性

12.2 μM IC50

manufacturer/tradename

Calbiochem®

保管条件

OK to freeze
protect from light

色

off-white

溶解性

DMSO: 100 mg/mL

保管温度

−20°C

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PKC Activator VII, CGK062

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CHK2 (I157T), active

assay

≥98% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

-

form

solid

form

powder

form

solid

form

-

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Upstate®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

-

color

off-white

color

white

color

yellow-white

color

-

solubility

DMSO: 100 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

solubility

-

詳細

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).

生物化学的／生理学的作用

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

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