HDAC6 Inhibitor II, BRD9757

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.

Cell permeable: yes

Primary Target
HDAC6

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Wagner, F.F., et al. 2013. J. Med. Chem.56, 1772.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)