Shopping Cart
- Remove All
- Your shopping cart is currently empty
Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $77 | In Stock | |
5 mg | $265 | In Stock | |
10 mg | $496 | In Stock | |
25 mg | $813 | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $418 | In Stock |
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&IC50 | HDAC6 (cell-free assay):4nM |
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. |
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. |
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. |
Animal Research | Animal Models: Athymic nude mice implanted with angioreactorsFormulation: DMSODosages: --Administration: Tubacin is filled in semiclosed angioreactors, and then implanted into the mice. |
Molecular Weight | 721.86 |
Formula | C41H43N3O7S |
Cas No. | 537049-40-4 |
Smiles | S(C[C@@H]1O[C@@H](O[C@@H](C1)C2=CC=C(CO)C=C2)C3=CC=C(NC(CCCCCCC(NO)=O)=O)C=C3)C4=NC(=C(O4)C5=CC=CC=C5)C6=CC=CC=C6 |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 93 mg/mL (128.8 mM) Ethanol: <1 mg/mL H2O: <1 mg/mL | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.