AM 114

AM 114

Catalog Number:
L002369374APE
Mfr. No.:
APE-A8163
Price:
$180
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      • Overview
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          Background

          AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 μM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. AM 114 also exerts anti-cancer activity against cancer cells, which potently inhibits the growth of human colon cancer HCT116 cells with values of IC50 of 1.5 μM and 0.6 μM in MTT and colony formation assays respectively.

      • Properties
        • Alternative Name
          [4-[(Z)-[(5Z)-5-[(4-boronophenyl)methylidene]-1-methyl-4-oxopiperidin-3-ylidene]methyl]phenyl]boronic acid
          CAS Number
          856849-35-9
          Molecular Formula
          C20H21B2NO5
          Molecular Weight
          377.01
          Appearance
          A solid
          Purity
          96.36%
          Solubility
          insoluble in H2O; ≥16.65 mg/mL in DMSO; ≥4.11 mg/mL in EtOH with ultrasonic
          Storage
          Store at 4°C

          * For Research Use Only

      • Reference
        • 1. Gunderwala A, Porter J. "A luminescence assay for natural product inhibitors of the Mycobacterium tuberculosis proteasome." Phytochem Anal. 2016 Mar;27(2):126-32. PMID:26778282
          2. Chen, Wei, et al. "Competitive Expression of Endogenous Wheat CENH3 May Lead to Suppression of Alien ZmCENH3 in Transgenic Wheat× Maize Hybrids." Journal of Genetics and Genomics (2015).

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