| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
HDAC1 (IC50 = 0.7 nM); HDAC2 (IC50 = 1 nM); HDAC3 (IC50 = 2 nM); HDAC6 (IC50 = 9.3 nM)
Crebinostat targets class I HDAC1/2/3 and class IIb HDAC6. It is a potent HDAC inhibitor with IC50 values of 0.7 nM for HDAC1, 1.0 nM for HDAC2, 2.0 nM for HDAC3, and 9.3 nM for HDAC6. It shows weaker inhibition of the class I HDAC8 and no significant inhibition of the class IIa HDAC4/5/7/9. |
|---|---|
| ln Vitro |
Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells[1].
Crebinostat (1 μM; 24 h) upregulates Bdnf and Hspa1b (Hsp70) mRNA expression while downregulating Mapt mRNA expression in mouse primary cultured neurons[1]. Crebinostat (1 μM; 24 h) raises synapsin and histone acetylation. In primary cultured neurons, I punctae are found along dendrites[1]. Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neurons, with EC50 values of 0.29 μM and 0.18 μM, respectively. It downregulates Mapt mRNA expression and upregulates Hspa1b (Hsp70) and Bdnf in mouse primary cultured neurons. Crebinostat increases the density of synapsin-1 punctae along dendrites in neurons in vitro. |
| ln Vivo |
Crebinostat (25 mg/kg; IP; for 10 days) increases the amount of H4K12 and H3K9 acetylation in the entire hippocampus and improves mice's memory of contextual fear conditioning[1]. |
| Enzyme Assay |
Crebinostat is evaluated in cell-free HDAC enzyme activity assays. The compound is incubated with purified HDAC enzymes (HDAC1, HDAC2, HDAC3, HDAC6) and a fluorogenic substrate. The inhibition of deacetylase activity is measured by fluorescence detection. IC50 values are determined to quantify the potency of HDAC inhibition.
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| Cell Assay |
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. Crebinostat is assessed in cell-based assays using mouse primary neurons. Cells are treated with Crebinostat (1 μM; 24 h), and histone acetylation (AcH4K12 and AcH3K9) is measured using Western blot analysis. The expression of Mapt, Hspa1b, and Bdnf is measured by qPCR. The density of synapsin-1 punctae along dendrites is assessed by immunocytochemistry. |
| Animal Protocol |
Male C57BL/6J mice (9-10 weeks)[1]
25 mg/kg IP; alternate daily between left and right sides of the abdomen, for 10 days Crebinostat is administered in mouse models to evaluate its effects on memory and neuroplasticity. It modulates chromatin-mediated neuroplasticity and enhances memory. Efficacy is assessed using behavioral tests and by measuring histone acetylation and gene expression in brain tissues. |
| ADME/Pharmacokinetics |
Crebinostat has a molecular weight of 336.39 and a molecular formula of C19H16N2O4. It has a CAS number of 1092061-61-4. The compound is a white to off-white solid powder. It should be stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Crebinostat. The compound is for research use only and is not intended for human therapeutic use. It has shown neuroprotective effects in preclinical models.
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| References | |
| Additional Infomation |
N'-hydroxy-N-[(4-phenylphenyl)methyleneamino]heptanamide is a member of the biphenyl class of compounds.
Crebinostat is a potent, broad-spectrum HDAC inhibitor. It is a novel cognitive enhancer. It has anticancer and neuroprotective effects. The compound is not approved for clinical use. |
| Molecular Formula |
C20H23N3O3
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|---|---|
| Molecular Weight |
353.414924860001
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| Exact Mass |
353.173
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| Elemental Analysis |
C, 67.97; H, 6.56; N, 11.89; O, 13.58
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| CAS # |
1092061-61-4
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| Related CAS # |
1092061-61-4
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| PubChem CID |
25118059
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.583
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| LogP |
2.87
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
26
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| Complexity |
453
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCCCCC(NO)=O)N/N=C\C1C=CC(=CC=1)C1C=CC=CC=1
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| InChi Key |
AEIVDBATQVVQFS-RCCKNPSSSA-N
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| InChi Code |
InChI=1S/C20H23N3O3/c24-19(9-5-2-6-10-20(25)23-26)22-21-15-16-11-13-18(14-12-16)17-7-3-1-4-8-17/h1,3-4,7-8,11-15,26H,2,5-6,9-10H2,(H,22,24)(H,23,25)/b21-15+
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| Chemical Name |
N'-hydroxy-N-[(E)-(4-phenylphenyl)methylideneamino]heptanediamide
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| Synonyms |
Crebinostat
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~282.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8296 mL | 14.1479 mL | 28.2957 mL | |
| 5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8296 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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