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Butyrolactone 3

Catalog No.GC10226

histone acetyltransferase Gcn5 inhibitor

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Butyrolactone 3 Chemical Structure

Cas No.: 778649-18-6

Size Price Stock Qty
1mg
$75.00
In stock
5mg
$217.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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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.

Reference:
1.  M. Biel, A. Kretsovali, E. Karatzali, et al. Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5. Angewandte Chemie International Edition 43, 3974-3976 (2004).

Chemical Properties

Cas No. 778649-18-6 SDF
Chemical Name rel-tetrahydro-4-methylene-5-oxo-2R-propyl-3S-furancarboxylic acid
Canonical SMILES O=C1C([C@@H](C(O)=O)[C@H](CCC)O1)=C
Formula C9H12O4 M.Wt 184.2
Solubility ≤14mg/ml in ethanol;14mg/ml in DMSO;13mg/ml in dimethyl formamide Storage Store at -20°C,unstable in solution, ready to use.
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 5.4289 mL 27.1444 mL 54.2888 mL
5 mM 1.0858 mL 5.4289 mL 10.8578 mL
10 mM 0.5429 mL 2.7144 mL 5.4289 mL
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