product name BRD73954
Description: BRD73954 is a potent and selective HDAC inhibitor with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively. Also, BRD73954 inhibited HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC7 and HDAC9 with IC50 values of 12, 9.0, 23, >33, >33, 13 and >33 μM, respectively. In HeLa cells, BRD73954 significantly increased α-tubulin acetylation, which was a substrate for HDAC6, while there was no change in the acetylation state of histone H3, which was a substrate for HDACs 1, 2 and 3.
References: J Med Chem. 2013 Jun 13;56(11):4816-20.
284.31
Formula
C16H16N2O3
CAS No.
1440209-96-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 56 mg/mL (197.0 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL warmed (9.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424436
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2013 Jun 13;56(11):4816-20. |
