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A dihydropyrazol derivative that acts as a selective activator of eukaryotic translation initiation factor 2-alpha kinase 3 (EIF2AK3/PERK) and increases the phosphorylation of EIF2A at Ser51 in HT29 and MCF7 cells. Does not inhibit the activity of cyclin dependent kinases, but causes a rapid loss of cyclin D expression. Also shown to block Rb protein phosphorylation (EC50 = 4.2 µM) in HT29 cells. Reported to sensitize cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. Induces a long-term inhibition of cell proliferation even after its removal (GI50 = 3.1 µM).
EIF2AK3 Activator, CCT020312 - CAS 324759-76-4 - Calbiochem 分析证书
标题
批号
324879
参考
参考信息概述
Stockwell, S. R., et al. 2011. Plos One In press.
数据表
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.
A dihydropyrazol derivative that acts as a selective activator of eukaryotic translation initiation factor 2-alpha kinase 3 (EIF2AK3/PERK) and increases the phosphorylation of EIF2A at Ser51 in HT29 and MCF7 cells. Does not inhibit the activity of cyclin dependent kinases, but causes a rapid loss of cyclin D expression. Also shown to block Rb protein phosphorylation (EC50 = 4.2 µM) in HT29 cells. Reported to sensitize cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. Induces a long-term inhibition of cell proliferation even after its removal (GI50 = 3.1 µM).
Form
Yellowish-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
324759-76-4
Chemical formula
C₃₁H₃₀Br₂N₄O₂
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
-20°C
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.