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Tubacin

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

Catalog No. T6327Cas No. 537049-40-4

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Purity:98.71%

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COA HPLC HNMR

Tubacin

Catalog No. T6327Cas No. 537049-40-4

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
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

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Product Introduction

Bioactivity

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.

Chemical Properties

Molecular Weight	721.86
Formula	C₄₁H₄₃N₃O₇S
Cas No.	537049-40-4

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.3853 mL	6.9266 mL	13.8531 mL	69.2655 mL
5 mM	0.2771 mL	1.3853 mL	2.7706 mL	13.8531 mL
10 mM	0.1385 mL	0.6927 mL	1.3853 mL	6.9266 mL
20 mM	0.0693 mL	0.3463 mL	0.6927 mL	3.4633 mL
50 mM	0.0277 mL	0.1385 mL	0.2771 mL	1.3853 mL
100 mM	0.0139 mL	0.0693 mL	0.1385 mL	0.6927 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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