General description
A cell-permeable, low molecular weight hydroxamate compound that acts as a potent histone deacetylase class IIb HDAC6-selective inhibitor (IC50 = 30 nM), while inhibiting class I HDAC1/2/3/8 only at higher concentrations (IC50 = 0.638, 1.79, 0.694, and 1.09 µM, respectively) and exhibiting much reduced or little potency against class IIa HDAC4/5/7/9 (IC50 = 21.80, 18.32, 12.61, and >33.33 µM, respectively). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation level in HeLa cells (10 & 30 µM; 24 h) without inducing detectable histone H3 acetylation increase seen in cells treated with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187) or the general HDAC inhibitor SAHA. BRD9757 does not contain an apparent selectivity-imparting capping structure linked to the zinc-binding hydroxamate as seen in other ZBG- (Zinc binding group) containing HDAC inhibitors.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HDAC6
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Wagner, F.F., et al. 2013. J. Med. Chem.56, 1772.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥98% (HPLC) |
| Quality Segment | 100 |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | pale orange |
| solubility | DMSO: 100 mg/mL |
| storage temp. | 2-8°C |
