Quality Level
assay
≥98% (TLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
ethanol: 10 mg/mL, DMSO: 5 mg/mL, methanol: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
InChI
1S/C18H39NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-18(21)17(19)16-20/h17-18,20-21H,2-16,19H2,1H3
InChI key
OTKJDMGTUTTYMP-UHFFFAOYSA-N
General description
A cell-permeable and reversible lyso-sphingolipid protein kinase C (PKC) inhibitor that competitively interacts at the regulatory phorbol binding domain of PKC. Inhibits enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC (IC50 = 37.5 µM and 31 µM, respectively). Inhibits human PKCα, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC50 = 40 µM). Enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC; Cat. Nos. 47589 and 475820) in gastric cancer cells by promoting drug-induced apoptosis.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC
Enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC
Product does not compete with ATP.
Reversible: yes
Target IC50: 37.5 µM and 31 µM, inhibiting enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC, respectively
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kedderis, L.B., et al. 1995. Fundam. Appl. Toxicol.25, 201.
Sachs, C.W., et al. 1995. J. Biol. Chem. 270, 26639.
Schwartz, G.K., et al. 1995. J. Natl. Cancer Inst.87,1394.
Sachs, C.W., et al. 1995. J. Biol. Chem. 270, 26639.
Schwartz, G.K., et al. 1995. J. Natl. Cancer Inst.87,1394.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 559300-1MG | 04055977192407 |