Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
University of Otago. 2019.
Transcriptional effects of mood stabiliser drugs in a serotonergic cell line
Tubastatin A purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | normal human (i.e., H69) and rat (NRC) cholangiocyte cell lines |
| Preparation method | Proliferation assays Proliferation assays were conducted using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay (MTS; Promega) and/or counting cells using the Cellometer Auto4 (Nexcelom Bioscience) cell counter. |
| Concentrations | 0, 4 µ M |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | orthotopic, syngeneic CCA model in rats |
| Formulation | saline |
| Dosages | 10 mg/kg daily for 7 days |
| Administration | intraperitoneally |
| Molecular Weight | 335.4 |
| Formula | C20H21N3O2 |
| CAS Number | 1252003-15-8 |
| Solubility (25°C) | DMSO 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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