Crebinostat

SKU: orb1941111

Description

Crebinostat is a novel cognitive enhancer that inhibits class I HDAC/1/2/3 (IC50=0.7/1.0/2.0 nM), class IIb HDAC6 (IC50=9.3 nM) with weaker inhibition of the class I HDAC8 and no significant inhibition of the class IIa HDAC/4/5/7/9; potently induces acetylation of both histone H3 and histone H4 as well as enhanced the expression of the CREB target gene Egr1 in cultured mouse primary neurons; upregulates Bdnf and Grn, and downregulates Mapt (tau) gene expression-genes; brain penetrant.(In Vitro):Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells.Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons.Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons.(In Vivo):Crebinostat (25 mg/kg; IP; for 10 days) enhances memory of contextual fear conditioning in mice; induces an increase in total hippocampal acetylation of H4K12 and H3K9.

Key Properties

• CAS Number: 1092061-61-4
• MW: 353.422
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₃N₃O₃
• SMILES: O=C(NO)CCCCCC(N/N=C/C1=CC=C(C2=CC=CC=C2)C=C1)=O
• Target: HDAC
• Solubility: In Vitro: DMSO : 100 mg/mL (282.96 mM)

Bioactivity

• In Vivo:
  Crebinostat (25 mg/kg; IP; for 10 days) enhances memory of contextual fear conditioning in mice; induces an increase in total hippocampal acetylation of H4K12 and H3K9. Animal model: Male C57BL/6J mice (9-10 weeks). Dosage: 25 mg/kg. Administration: IP; alternate daily between left and right sides of the abdomen, for 10 days. Result: Enhanced memory of contextual fear conditioning in mice; induced a trend towards an increase in total hippocampal acetylation of both 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. Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA expression in mouse primary cultured neurons. Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons. Western blot analysis. Cell line: Mouse primary neuronal cells (dissociated from E17 embryonic mouse forebrain). Concentration: 1 μM. Incubation time: 24 h. Result: Induced robust acetylation of AcH4K12 and AcH3K9 in a dose dependent manner with EC50s of 0.29 μM and 0.18 μM.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Crebinostat

Quick Database Links

Gene Symbol

HDAC