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Tubastatin A

Catalog No. T1966   CAS 1252003-15-8
Synonyms: Tubastatin A BASE

Tubastatin A (Tubastatin A BASE) is an effective and specific HDAC6 inhibitor (IC50: 15 nM, in a cell-free assay). Its selectivity is 1000-fold against all the other isozymes except HDAC8.

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Tubastatin A Chemical Structure
Tubastatin A, CAS 1252003-15-8
Pack Size Availability Price/USD Quantity
10 mg In stock $ 41.00
25 mg In stock $ 58.00
50 mg In stock $ 72.00
100 mg In stock $ 113.00
200 mg In stock $ 172.00
500 mg In stock $ 288.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
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Purity: 99.51%
Purity: 98.36%
Purity: 98.32%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tubastatin A (Tubastatin A BASE) is an effective and specific HDAC6 inhibitor (IC50: 15 nM, in a cell-free assay). Its selectivity is 1000-fold against all the other isozymes except HDAC8.
Targets&IC50 HDAC6:15 nM
Kinase Assay HDAC enzymatic assays: Tubastatin A is dissolved and diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine) to 6-fold of the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with Tubastatin A for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.
Cell Research Anchorage-independent growth is assessed by growing cells in soft agar. About 25,000 cells suspended in 0.4% agar in culture media are layered over a 1% agar layer in a 6-well plate. Media are added twice a week and pictures are taken after 21 days of incubation. The number and size of colonies are analyzed using the Gel-Pro software.(Only for Reference)
Synonyms Tubastatin A BASE
Molecular Weight 335.4
Formula C20H21N3O2
CAS No. 1252003-15-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62 mg/mL (184.9 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Butler KV, et al. J Am Chem Soc, 2010, 132(31), 10842-10846. 2. Gradilone SA, et al. Cancer Res, 2013, 73(7), 2259-2270. 3. Vishwakarma S, et al. Int Immunopharmacol, 2013, 16(1), 72-78. 4. Santo L, et al. Blood, 2012, 119(11), 2579-2589.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library Reprogramming Compound Library Histone Modification Compound Library DNA Damage & Repair Compound Library Epigenetics Compound Library Anti-Aging Compound Library Apoptosis Compound Library Autophagy Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

Tubastatin A 1252003-15-8 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Inhibitor inhibit Histone deacetylases Tubastatin A BASE inhibitor

 

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