100082
14-3-3 Antagonist II, BV02
2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
31 May 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | Off-white powder | ||
| Molar mass | 395.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C20H17N3O6 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Regulatory Review |
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