| Name | Tubacin |
| 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. |
| Cell Research | 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. |
| Kinase Assay | 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. |
| Animal Research | Animal Models: Athymic nude mice implanted with angioreactorsFormulation: DMSODosages: --Administration: Tubacin is filled in semiclosed angioreactors, and then implanted into the mice. |
| 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. Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (4.57 mM), Sonication is recommended.
DMSO : 50 mg/mL (69.27 mM), Sonication is recommended.
Ethanol : <1 mg/mL
H2O : <1 mg/mL
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| Keywords | VirusProtease | Virus Protease | Tubacin | Inhibitor | inhibit | Histone deacetylases | HDAC6 | HDAC |
| Inhibitors Related | Neomycin sulfate | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Doxycycline | Manganese chloride (tetrahydrate) | Thymidine | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate |
| Related Compound Libraries | Reprogramming Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | HIF-1 Signaling Pathway Compound Library | Hematonosis Compound Library | Protease Inhibitor Library | Anti-Viral Compound Library | Inhibitor Library | Anti-Bacterial Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
