| Field | Specification |
|---|---|
| Target | |
| Alternative names | EKZ-001 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H27FN2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Bavarostat, also known as EKZ-001, crosses the blood-brain barrier and acts as both an HDAC6 inhibitor and a PET radiotracer, reaching an IC50 as low as 17 nM against human HDAC6. It can be labeled with 18F and used as a probe for mapping HDAC6 distribution and measuring target occupancy in non-human primate brains. The compound selectively affects tubulin acetylation while leaving histone acetylation unchanged, and it is applied in research on Alzheimer's disease, other neurodegenerative disorders, and cancers[1][2][3]. It is supplied as a light yellow to yellow solid (C20H27FN2O2, MW 346.44) at 99.51% purity.
Physical & Chemical Properties
| CAS Number | 2134109-20-7 |
|---|---|
| Molecular Formula | C20H27FN2O2 |
| Molecular Weight | 346.44 g/mol |
| Purity | 99.51% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C(NO)C1=CC=C(CN(C)CC2(C3)CC4CC3CC(C4)C2)C(F)=C1 |
| Target | HDAC6, HDAC9, HDAC7, HDAC8, HDAC4, HDAC5, HDAC11, HDAC1, HDAC2, HDAC3 |
| Signaling Pathway | Cell Cycle/DNA Damage; Epigenetics; Cytoskeleton |
| Solubility | In Vitro: DMSO: 100 mg/mL (288.65 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
|
HDAC6 0.06 μM (IC50) |
HDAC9 5.2 μM (IC50) |
HDAC7 4.7 μM (IC50) |
HDAC8 8.5 μM (IC50) |
HDAC4 11.3 μM (IC50) |
HDAC5 19 μM (IC50) |
HDAC11 10 μM (IC50) |
HDAC1 >1000 μM (IC50) |
HDAC2 >1000 μM (IC50) |
HDAC3 >1000 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Rahal D. Translation of HDAC6 PET imaging using [18F] EKZ-001–cGMP production and measurement of HDAC6 target occupancy in NHPs–A Review[J]. 2022.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (288.65 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (7.22 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (7.22 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In baboon cerebellum tissue in vitro, EKZ-001 (Bavarostat) (10 μM; 30 min pre-incubation) completely blocks the binding of [18F]EKZ-001 to HDAC6, with a blocking efficiency of 100 ± 10% at 10 μM[1].
In Vivo
In the healthy baboon brain, pre-treatment with a single i.v. dose of non-radioactive EKZ-001 (0.1-1 mg/kg) achieves ≥85% HDAC6 target occupancy[1].
| Animal Model | Baboon (female)[1] |
|---|---|
| Dosage | 0.1 mg/kg; 1 mg/kg |
| Administration | i.v.; single dose; pre-treatment |
| Result | Achieved ≥85% HDAC6 target occupancy in the brain. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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