Butyrolactone 3

Butyrolactone 3

Catalog Number:
L002372770APE
Mfr. No.:
APE-C3209
Price:
$196
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      • Overview
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          Background

          IC50: 100 μM
          Butyrolactone 3 is a histone acetyltransferase Gcn5 inhibitor.
          The human histone acetyltransferase Gcn5 is identified as a prominent member of the GNAT family with high preference for histone H3 as a substrate.
          In vitro: The analogs of butyrolactone 3 only showed a weak inhibition of CBP, while butyrolactone 3 led to an inhibition of Gcn5. It was important to see that in the presence of acetyl-CoA the Kd value for binding of histone H3 to Gcn5 or PCAF was around 100 mM. Moreover, the affinity of butyrolactone 3 to the Gcn5 enzyme was found to be comparable to that of the natural substrate H3 and could provide an good starting point for the study of SAR. In addition, a nonirreversible inhibition of Gcn5 could be determine, and thus a Michael addition of nucleophilic groups of the enzymeBs active side was unlikely. Therefore, the derivatization of gbutyrolactone 3 at position 2 might be a promising starting point for future SAR studies [1].
          In vivo: So far, there is no animal in vivo data reported.
          Clinical trial: Up to now, Butyrolactone 3 is still in the preclinical development stage.

      • Properties
        • Alternative Name
          rel-tetrahydro-4-methylene-5-oxo-2R-propyl-3S-furancarboxylic acid
          CAS Number
          778649-18-6
          Molecular Formula
          C9H12O4
          Molecular Weight
          184.2
          Appearance
          A crystalline solid
          Purity
          Purity ≥95.00%
          Solubility
          ≤14mg/ml in ethanol;14mg/ml in DMSO;13mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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