Crebinostat

SKU: orb1700803

Description

Crebinostat is a potent HDAC inhibitor targeting HDAC1, HDAC2, HDAC3, and HDAC6. It induces histone acetylation, modulates synaptic plasticity in vitro, and enhances memory in vivo by upregulating CREB target genes like Egr1.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1092061-61-4
• MW: 353.41
• Purity: 94.96% (May vary between batches)
• Formula: C₂₀H₂₃N₃O₃
• SMILES: C(=NNC(CCCCCC(NO)=O)=O)C1=CC=C(C=C1)C2=CC=CC=C2
• Target: Histone Acetyltransferase,HDAC,Epigenetic Reader Domain
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.83 mM);DMSO:0.88 mg/mL (2.49 mM)

Bioactivity

• Target IC50:
  HDAC2:1.0 nM|HDAC3:2.0 nM|HDAC1:0.7 nM|HDAC6:9.3 nM
• In Vivo:
  Crebinostat (25 mg/kg; i.p.; for 10 days; Male C57BL/6J mice) boosts memory in mice during contextual fear conditioning and leads to a rise in overall hippocampal acetylation of H4K12 and H3K9.
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• In Vitro:
  Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells, with EC50 values of 0.29 μM and 0.18 μM, respectively. It downregulates Mapt mRNA expression and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression, while increasing histone acetylation and synapsin I punctae along dendrites in primary cultured neurons.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Crebinostat, CREB, HDAC, HistoneAcetyltransferase, Histone Acetyltransferase, histone acetyltransferase, EpigeneticReaderDomain, Epigenetic Reader Domain

Compound Identifiers

PubChem CID

91110942