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48-602MAG
Buffer Detection Kit for Magnetic Beads
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504045
Sigma-AldrichFocal Adhesion Kinase Inhibitor III - CAS 1426683-53-5 - Calbiochem
A cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 µM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.
Catalogue Number
504045
Brand Family
Calbiochem®
Synonyms
FAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
References
References
Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett.23, 1779.
Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett.23, 1779.
Data Sheet
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.
Revision
17-July-2013 JSW
Synonyms
FAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide
Description
A cell-permeable pyrazolobenzothiazinedioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition against FAK kinase activity in cell-free assays (IC50 = 0.64 and 2.2 µM, respectively, with 60 or 5 min FAK-inhibitor preincubation before substrate poly-GT and 0.5 µM ATP addition) and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1 µM with 30 min inhibitor preincubation before 2 h stimulation by plating cells on fibronectin-coated surface), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38α, Pyk2, or Src even at concentrations as high as 10 µM.
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1426683-53-5
Chemical formula
C₂₂H₂₆N₄O₂S
Structure formula
Purity
≥99% 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.
Toxicity
Standard Handling
References
Tomita, N., et al. 2013. Bioorg. Med. Chem. Lett.23, 1779.
