General description
A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50 = 600 nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50 = 1 to 2.5 µM) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model.
A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50 = 600 nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50 = 1 to 2.5 mM) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model.
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
Lee, S., et al. 2011. J. Med. Chem.54, 6364
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 533.59. Empirical Formula: C30H30F3N5O. Quality Level: 100. Assay: ≥. 94% (HPLC). form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 407331-5MG