BRD73954

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Technical Data

Molecular Weight 284.31 Storage powder
Formula

C16H16N2O3

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CAS No. 1440209-96-0 Synonyms N/A
Solubility (25°C) * In vitro DMSO 56 mg/mL (196.96 mM)
Ethanol 9 mg/mL warmed (31.65 mM)
Water Insoluble
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N1-hydroxy-N3-phenethylisophthalamide

Biological Activity

Description BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
Targets
HDAC6 [1]
()
HDAC8 [1]
36 nM 120 nM
In vitro As compared to the other class I and II histone deacetylases (HDACs) (HDAC1, 12 μM; HDAC2, 9 μM; HDAC3, 23μM; HDAC4, >33 μM; HDAC5, >33 μM; HDAC7, 13 μM; HDAC8, 120 nM; HDAC9, >33 μM), BRD73954 maintains excellent selectivity toward HDAC6 and HDAC8 with IC50 of 36 nM and 120 nM, respectively. Treatment with BRD73954 results in a robust increase in α -tubulin acetylation. [1]
In vivo
Features  

Protocol (Only for Reference)

Kinase Assay: [1]

HDAC inhibition assay Purified HDACs are incubated with 2 µM carboxyfluorescein(FAM)-labeled acetylated or trifluoroacetylated peptide substrate and test compound for 60 min at room temperature, in HDAC assay buffer that contained 50 mM HEPES (pH 7.4), 100 mM KCl, 0.01% BSA and 0.001% Tween-20. Reactions are terminated by the addition of the known pan HDAC inhibitor LBH-589 with a final concentration of 1.5 µM. Substrate and product are separated electrophoretically and fluorescence intensity in the substrate and product peaks is determined and analyzed by Labchip EZ Reader. IC50 values are automatically calculated by Origion8 using 4 Parameter Logistic Model. The percent inhibition is plotted against the compound concentration, and the IC50 values are automatically fitted by Genedata Screener software using 4-parameter logistic dose response model.
 

References

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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