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324879 Sigma-Aldrich

EIF2AK3 Activator, CCT020312 - Calbiochem

The EIF2AK3 Activator, CCT020312 modulates the biological activity of EIF2AK3.

Synonym: 6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one, PERK activator, CCT020312, EIF2AK3 Activator, CCT020312 - Calbiochem

  • Empirical Formula (Hill Notation) C31H30Br2N4O2

  • Molecular Weight 650.40

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Properties

assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   yellow-white
solubility   DMSO: 50 mg/mL
shipped in   ambient

Description

General description

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).

Packaging

5 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Stockwell, S. R., et al. 2011. Plos One In press.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.

Documents

Certificate of Analysis (COA)

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