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Purity: ≥98%
Tubacin (known also as tubulin acetylation inducer) is a specific HDAC6 (histone deacetylase 6) inhibitor with potential anticancer activity. In a cell-free assay, it inhibits HDAC6 with an IC50 of 4 nM and shows approximately ~350-fold higher selectivity for HDAC6 than HDAC1.
| Targets |
HDAC6 ( IC50 = 4 nM ); HDAC3 ( IC50 = 1.27 μM ); HDAC8 ( IC50 = 1.27 μM ); HDAC1 ( IC50 = 1.40 μM ); HDAC5 ( IC50 = 3.35 μM ); HDAC10 ( IC50 = 3.71 μM ); HDAC11 ( IC50 = 3.79 μM ); HDAC9 ( IC50 = 4.31 μM ); HDAC2 ( IC50 = 6.27 μM ); HDAC7 ( IC50 = 9.70 μM ); HDAC4 ( IC50 = 17.30 μM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The Reaction Biology HDAC Spectrum platform is utilized for the execution of enzyme inhibition experiments. Isolated recombinant human protein was utilized in the HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays; the HDAC3/NcoR2 complex is utilized in the HDAC3 test. Fluorogenic peptide derived from p53 residues 379–382 (RHKKAc) serves as the substrate for HDAC1, 2, 3, 6, 10, and 11 assays; fluorogenic diacyl peptide derived from p53 residues 379–382 (RHKAcKAc) serves as the substrate for HDAC8. For HDAC4, 5, 7, and 9 assays, acetyl-Lys(trifluoroacetyl)-AMC substrate is utilized. After dissolving compounds in DMSO, they are tested in 10-dose IC50 mode using a 3-fold serial dilution protocol that begins at 30 μM. Trichostatin A (TSA), the control compound, is tested in a 10-dose IC50 using a 3-fold serial dilution that begins at 5 μM. Curve-fitting the dose/response slopes yields IC50 values.
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| Cell Assay |
The assay uses tubacin, TBSA, VPA, and TSA as HDAC inhibitors. TE671 and BHK-21 cells are used to test the cytotoxicity of HDACi using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. In 96-well plates, 5 × 104 cells are seeded per well, and each HDACi is then added at the indicated concentration. Following a 48-hour treatment period, each well receives 25 μL of MTT solution (5 mg/mL), which is then incubated for three hours at 37 °C with 5% CO2. To dissolve formazan crystals, 100 μL of DMSO is added to each well following three washes with phosphate buffer saline (PBS). The micro-ELISA reader measures OD570−630, and the survival rate is computed to show the inhibitory effects of each HDACi on the viability of BHK-21 and TE671 cells. ((Acontrol − Aexperiment)/Acontrol) × 100% is the survival rate (%). The values of the 50% cytotoxic concentration (CC50) are determined by computer programs.
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| Animal Protocol |
Athymic nude mice implanted with angioreactors
Tubacin is filled in semiclosed angioreactors, and then implanted into the mice. |
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| References |
| Molecular Formula |
C41H43N3O7S
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| Molecular Weight |
721.86
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| Exact Mass |
721.28
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| Elemental Analysis |
C, 68.22; H, 6.00; N, 5.82; O, 15.51; S, 4.44
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| CAS # |
537049-40-4
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1[C@@H](O[C@@H](O[C@@H]1C2=CC=C(C=C2)CO)C3=CC=C(C=C3)NC(=O)CCCCCCC(=O)NO)CSC4=NC(=C(O4)C5=CC=CC=C5)C6=CC=CC=C6
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| InChi Key |
BHUZLJOUHMBZQY-YXQOSMAKSA-N
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| InChi Code |
InChI=1S/C41H43N3O7S/c45-26-28-17-19-29(20-18-28)35-25-34(27-52-41-43-38(30-11-5-3-6-12-30)39(51-41)31-13-7-4-8-14-31)49-40(50-35)32-21-23-33(24-22-32)42-36(46)15-9-1-2-10-16-37(47)44-48/h3-8,11-14,17-24,34-35,40,45,48H,1-2,9-10,15-16,25-27H2,(H,42,46)(H,44,47)/t34-,35+,40+/m1/s1
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| Chemical Name |
N-[4-[(2R,4R,6S)-4-[(4,5-diphenyl-1,3-oxazol-2-yl)sulfanylmethyl]-6-[4-(hydroxymethyl)phenyl]-1,3-dioxan-2-yl]phenyl]-N'-hydroxyoctanediamide
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| Synonyms |
Tubacin; tubulin acetylation inducer
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3853 mL | 6.9266 mL | 13.8531 mL | |
| 5 mM | 0.2771 mL | 1.3853 mL | 2.7706 mL | |
| 10 mM | 0.1385 mL | 0.6927 mL | 1.3853 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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