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MBIMPH Fluorinated Analog 1; 3-Fluoro-N-hydroxy-4-((2-methyl-1H-benzo[d]imidazol-1-yl)methyl)benzamide

Chemical

C16H14FN3O2 . HCl

299.3 . 36.5

≥95% (HPLC)

Off-white solid.

Soluble in DMSO, ethanol, methanol or water.

Determined by 1H-NMR.

NWMOSGPUNITEFR-UHFFFAOYSA-N

AMBIENT

+4°C

-20°C

Keep cool and dry.Protect from light.

Stable for at least 2 years after receipt when stored at -20°C.

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• Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC₅₀ =3nM). Displays high selectivity over all other HDACs (IC₅₀=0.03-20µM).
• Induces cellular α-tubulin, but not histone H3 hyperacetylation in Neuro-2a cells. Promotes mitochondrial transport.
• Shows improved kinetics and biochemical potency against HDAC6 compared to tubastatin A (AG-CR1-3900).
• HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, H4). Histone deacetylases act via the formation of large multiprotein complexes. HDAC6 plays an important role in microtubule-dependent cell motility, transcriptional regulation, degradation of misfolded proteins and cell cycle and is involved in autophagy, inflammation, cancer and neurodegeneration.

Product References

Bicyclic-capped histone deacetylase 6 inhibitors with improved activity in a model of axonal charcot-marie-tooth disease: S. Shen, et al.; ACS Chemical Neuroscience (submitted) (2015)

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