HDAC6 Inhibitor II, BRD9757-CAS 1423058-85-9-Calbiochem

C₆H₉NO₂

127.14

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 potency against class IIa HDAC4/5/7/9 (IC₅₀ >12.61 µM). Shown to selectively upregulate HDAC6 substrate α-tubulin acetylation in HeLa cells (10 & 30 µM; 24 h) without inducing histone H3 acetylation increase seen with another HDAC6-selective inhibitor Tubastatin A (Cat. No. 382187). Unlike other Zinc-binding group-containing HDAC inhibitors, BRD9757 does not contain an apparent selectivity-imparting capping structure linked to its hydroxamate.
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

Toxicity: Standard Handling (A)

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

100

≥98% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

pale orange

DMSO: 100 mg/mL

2-8℃

Packaged under inert gas

GHS07

Warning

H319 - H412

P264 - P273 - P280 - P305 + P351 + P338 - P337 + P313 - P501

Aquatic Chronic 3 - Eye Irrit. 2

11 - Combustible Solids

WGK 3