5.05760

HDAC6 Inhibitor II, BRD9757

• Synonym(e): HDAC6 Inhibitor II, BRD9757, N-Hydroxycyclopent-1-enecarboxamide, HDAC Inhibitor XVI, Histone Deacetylase Inhibitor XVI
• Empirische Formel (Hill-System): C₆H₉NO₂
• CAS-Nummer: 1423058-85-8
• Molekulargewicht: 127.14
• MDL-Nummer: MFCD00004773
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: pale orange
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
HDAC6

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• H-Sätze: H319 - H412
• P-Sätze: P264 - P273 - P280 - P305 + P351 + P338 - P337 + P313 - P501
• Gefahreneinstufungen: Aquatic Chronic 3 - Eye Irrit. 2
• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable