Antibodies
Tubacin
- 貨號 Cat. No.
- S2239
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Tubacin
Catalog No.S22391 Product Citations
Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.
| Size | Price | Stock | Quantity | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1. | |||||
|---|---|---|---|---|---|---|
| Targets | HDAC6 | |||||
| IC50 | 4 nM [1] | |||||
| In vitro | Tubacin, without directly stabilizing microtubules, induces an increase in α-tubulin acetylation with EC50 of 2.5 μM in A549 cells. Tubacin inhibits HDAC6-mediated α-tubulin deacetylation, and inhibits the migration of both wild-type and HDAC6-overexpressing cells. [2] Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. [3] Tubacin significantly inhibits both drug-sensitive and drug–resistant MM cell growth with IC50 of 5–20 μM, and induces cell apoptosis by activation of caspases. [4] | |||||
| In vivo | In chick embryos, inhibition of HDAC6 activity by Tubacin reduces the formation of new blood vessels in matrigel/nylon mesh. In angioreactors implanted in mice, Tubacin also impairs the formation of new blood vessels. [5] | |||||
| Features | The first known selective inhibitor of α-tubulin deacetylation. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Enzyme Inhibition Assay | Enzyme inhibition assays are performed using the Reaction Biology HDAC Spectrum platform. The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays used isolated recombinant human protein; HDAC3/NcoR2 complex is used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10, and 11 assays is a fluorogenic peptide from p53 residues 379-382 (RHKKAc); substrate for HDAC8 is fluorogenic diacyl peptide based on residues 379-382 of p53 (RHKAcKAc). Acetyl-Lys(trifluoroacetyl)-AMC substrate is used for HDAC4, 5, 7, and 9 assays. Compounds are dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A (TSA) is tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values are extracted by curve-fitting the dose/response slopes. |
|---|
Cell Assay: [4]
| Cell lines | Drug-sensitive (MM.1S, U266, INA-6, and RPMI8226) and drug-resistant (RPMI-LR5 and RPMI-Dox40) MM cell lines |
|---|---|
| Concentrations | ~20 μM |
| Incubation Time | 72 hours |
| Method | The inhibitory effect of bortezomib and/or tubacin on MM cell growth is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance. All experiments are performed in quadruplicate. |
Animal Study: [5]
| Animal Models | Athymic nude mice implanted with angioreactors |
|---|---|
| Dosages | |
| Administration | Tubacin is filled in semiclosed angioreactors, and then implanted into the mice. |
References
Chemical Information
| Molecular Weight (MW) | 721.86 |
|---|---|
| Formula | C41H43N3O7S |
| CAS No. | 537049-40-4 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (138 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | N1-(4-((2R,4R,6S)-4-((4,5-diphenyloxazol-2-ylthio)methyl)-6-(4-(hydroxymethyl)phenyl)-1,3-dioxan-2-yl)phenyl)-N8-hydroxyoctanediamide |
|---|
Product Citations (1)
