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Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 values of 15 nM. Tubastatin A was substantially more selective than the known HDAC6 inhibitor Tubacin at all isozymes except HDAC8. In addition, Tubastatin A displayed over 1000-fold selectivity against all HDAC isoforms excluding HDAC8, where it displayed 54-fold selectivity. This compound displayed dose-dependent protection against HCA induced neuronal cell death starting at 5 μM with near complete protection at 10 μM.
| Cell Experiment | |
|---|---|
| Cell lines | Primary cortical neuron |
| Preparation method | Neuroprotection Assays Primary cortical neuron cultures were obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments were initiated 24 h after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells were rinsed with warm PBS and then placed in minimum essential medium (Invitrogen) containing 5.5 g/liter glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 µM cystine. Oxidative stress was induced by the addition of the glutamate analog homocysteate (HCA; 5 mM) to the media. HCA was diluted from 100-fold concentrated solutions that were adjusted to pH 7.5. In combination with HCA, neurons were treated with either TSA or Tubastatin A at the indicated concentrations. Viability was assessed after 24 h by MTT assay (3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide) method. |
| Concentrations | 0, 1, 2.5, 5.0, 7.5 and 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | dextran sodium sulfate (DSS) and adoptive transfer models of colitis |
| Formulation | DMSO |
| Dosages | 0.5 mg/kg of body weight/day |
| Administration | i.p |
| Molecular Weight | 371.86 |
| Formula | C20H21N3O2.HCl |
| CAS Number | 1310693-92-5 |
| Solubility (25°C) | DMSO: ≥ 11 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
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CM-444 is an inhibitor for HDAC and DNA methyltransferases (DNMT) with IC50 values of 6 nM-0.6 μM and 1.8-2.3 μM, respectively. CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models. |
| CM-1758
CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells. |
| T-518
T-518 is an orally active, selective, and blood-brain barrier permeable HDAC6 inhibitor with an IC50 value of 36 nM for human HDAC6. |
| SE-7552
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. |
| BRD9757
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. |
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