| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Tubastatin A (TubA, AG-CR13900), a tubacin derivative, is a potent and selective HDAC6 (Histone deacetylase 6) inhibitor (IC50 = 15 nM in a cell-free assay) with potential anticancer and anti-inflammatory activity. It showed that HDAC6 has the highest selectivity among the HDAC isoforms(excluding HDAC8 for which the IC50 is 0.9 μM), more than 1,000-fold.
| Targets |
HDAC6 ( IC50 = 15 nM ); HDAC8 ( IC50 = 854 nM ); HDAC1 ( IC50 = 16400 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
In the 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), tubastatin A is dissolved and diluted to six times the final concentration levels. Prior to adding the substrate, HDAC enzymes are diluted in assay buffer to 1.5 times the final concentration and pre-incubated for 10 minutes with tubastatin A. The enzymes' respective amounts of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) are calculated using a titration curve to determine the Michaelis constant (Km). Trypsin of sequencing grade 0.3 μM is used to dilute FTS or MAZ-1675 in assay buffer to a final concentration six times. The plate is put into a SpectraMax M5 microtiter plate reader after the substrate/trypsin mix has been added to the enzyme/compound mix and shaken for 60 seconds. Following the peptide substrate's lysine side chain's deacetylation, the enzymatic reaction is watched for the release of 7-amino-4-methoxy-coumarin over a 30-minute period. The reaction's linear rate is then computed.
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| Cell Assay |
Primary cortical neuron cultures are prepared, as previously mentioned, from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17). Twenty-four hours after plating, all experiments are started. Glutamate-mediated excitotoxicity cannot harm the cells in these circumstances. Cells are washed with warm PBS before being put in minimum essential medium with 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine for cytotoxicity investigations. The glutamate analogue homocysteate (HCA; 5 mM) is added to the media to cause oxidative stress. pH 7.5 solutions that are 100 times concentrated are used to dilute HCA. Tubastatin A is administered to neurons at the specified concentrations in addition to HCA. After a day, the MTT assay is used to determine viability.
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| References |
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| Additional Infomation |
Tubastatin A is a pyridoindole that is 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indole which is substituted on the tetrahydropyridine nitrogen by a methyl group and on the indole nitrogen by a p-[N-(hydroxy)aminocarbonyl]benzyl group. It is a histone deacetylase 6 (HDAC6) inhibitor that is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). It has a role as an EC 3.5.1.98 (histone deacetylase) inhibitor. It is a pyridoindole, a hydroxamic acid and a tertiary amino compound.
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| Molecular Formula |
C20H21N3O2
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| Molecular Weight |
335.4
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| Exact Mass |
371.14
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| Elemental Analysis |
C, 71.62; H, 6.31; N, 12.53; O, 9.54
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| CAS # |
1252003-15-8
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| Related CAS # |
1252003-15-8; 1239034-70-8 (TFA) ; 1252003-15-8 1310693-92-5 (HCl);
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| PubChem CID |
49850262
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| Appearance |
White solid powder
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| LogP |
3.125
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
478
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1
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| InChi Key |
GOVYBPLHWIEHEJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21N3O2/c1-22-11-10-19-17(13-22)16-4-2-3-5-18(16)23(19)12-14-6-8-15(9-7-14)20(24)21-25/h2-9,25H,10-13H2,1H3,(H,21,24)
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| Chemical Name |
N-hydroxy-4-[(2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)methyl]benzamide
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| Synonyms |
Tubastatin A hydrochloride; Tubastatin A HCl; TSA HCl; Tubastatin A; 1252003-15-8; Tubastatin-A; Tubastatin A (free base); Tubastatin A BASE; 2XTSOX1NF8; N-hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)methyl)benzamide; Tubastatin A(free base); Tubastatin A; TubA, AG-CR1-3900
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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 |
| 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) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4% DMSO+30% PEG 300: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9815 mL | 14.9076 mL | 29.8151 mL | |
| 5 mM | 0.5963 mL | 2.9815 mL | 5.9630 mL | |
| 10 mM | 0.2982 mL | 1.4908 mL | 2.9815 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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