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Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 332 € | In Stock | |
5 mg | 786 € | In Stock | |
10 mg | 1.073 € | In Stock | |
25 mg | 1.510 € | In Stock | |
50 mg | 1.881 € | In Stock | |
100 mg | 2.375 € | In Stock | |
500 mg | 4.655 € | In Stock |
Description | Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene. |
Targets&IC50 | HDAC1:0.7 nM, HDAC6:9.3 nM, HDAC2:1.0 nM, HDAC3:2.0 nM |
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.[1] |
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.[1] |
Molecular Weight | 353.41 |
Formula | C20H23N3O3 |
Cas No. | 1092061-61-4 |
Smiles | C(=NNC(CCCCCC(NO)=O)=O)C1=CC=C(C=C1)C2=CC=CC=C2 |
Relative Density. | 1.16 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: 1 mg/mL, Sonication is recommended. |
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