100082
14-3-3 Antagonist II, BV02 - Calbiochem
Synonym(s):
14-3-3 Antagonist II, BV02 - Calbiochem, 2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid
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About This Item
Empirical Formula (Hill Notation):
C20H17N3O6
Molecular Weight:
395.37
UNSPSC Code:
12352200
Assay
≥98% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable, non-peptidyl pyrazolylcarbamoyl compound that targets the amphipathic client protein-binding groove of 14-3-3 and effectively competes against cellular pro-apoptotic c-Abl and cell cycle inhibitor protein p27Kip1 (CDK inhibitor 1B) for 14-3-3ς interaction, leading to c-Abl mitochondrial membrane relocation, c-Abl and p27Kip1 nuclear translocation, sub-G1 arrest, enhanced c-Abl cleavage, caspase-9 and -8 activation (24 h 5 µM treatment), and eventual apoptotic cell death in pro-B murine Ba/F3 lines expressing wt, E255K, or T315I Bcr-Abl (LD50 = 0.41, 1.30, 1.47 µM, respectively;). Also demonstrated to exhibit antiproliferative activity against the survival of three primary IM- (Imatinib mesylate; STI571) resistant CD34+ cultures (LD50 = 0.5, 0.7, and 2.5 µM) from CML (chronic myeloid leukemia) patients with T315I Bcr-Abl mutation.
Packaging
Packaged under inert gas
Other Notes
Mancini, M., et al. 2011. J. Pharmacol. Exp. Ther.336, 596.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
Storage Class Code
10-13 - German Storage Class 10 to 13
Regulatory Information
监管及禁止进口产品
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