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
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 650.40. Empirical Formula: C31H30Br2N4O2. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: yellow-white. solubility: DMSO: 50 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. SMILES string: O: C1C(C2: NN(C(CCN(CC)CC): O)C(C3: CC: C(Br)C: C3)C2): C(C4: CC: CC: C4)C5: CC(Br): CC: C5N1. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51285402
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 324879-5MG