Tubastatin A HCl (Synonyms: TSA HCl;Tubastatin A hydrochloride) |
| Catalog No.GC10322 |
Tubastatin A HCl(Tubastatin A HCl)은 무세포 분석에서 IC50이 15nM인 강력하고 선택적인 HDAC6억제제이며 HDAC8(57배 이상)을 제외한 다른 모든 동종효소에 대해 선택적(1000배 이상)입니다. 투바스타틴 A HCl은 또한 HDAC10 및 메탈로-β-락타마제 도메인 함유 단백질2(MBLAC2)을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1310693-92-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Tubastatin A HCl is a selective inhibitor of HDAC6 with IC50 value of 15 nM [1].
HDAC6 (histone deacetylase 6) is an enzyme and plays an important role in a variety of processes, including transcriptional regulation, cell cycle preogression and developmental events. Abnormal expression of HDAC6 is correlated with many kinds of diseases, including Alzheimer's disease and cancers [1].
Tubastatin A HCl is a potent HDAC6 inhibitor and has the most selective compared with other HDAC isoforms. When tested with primary cortical neuron cells, Tubastatin A HCl treatment protected HCA-induced neuronal cell death in a dose range from 5 μM to 10 μM [1]. In HaCaT cells, administration of Tubastatin A HCl prevented sodium arsenite from inducing association of Nrf2 mRNA with ribosomes and elevation of Nrf2 protein by selectively inhibitng HDAC6 activity and had no effect on other HDACs [2]. Using atomic force microscopy study, Ketene AN et al. revealed that Tubastatin A HCl increased cell elasticity by inhibiting HDAC6 [3].
References:
[1]. Kyle V. Butler, Jay Kalin, Camille Brochier, et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A [J]. J. Am. Chem. Soc., 2010, 132 (31), pp 10842–10846.
[2]. Kappeler KV, Zhang J, Dinh TN, et al. Histone deacetylase 6 associates with ribosomes and regulates de novo protein translation during arsenite stress [J]. Toxicol Sci. 2012 May;127(1):246-255.
[3]. Ketene AN, Roberts PC, Shea AA, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells [J]. Integr Biol (Camb). 2012 May;4(5):540-549.
| Kinase experiment [1]: | |
|
Enzyme inhibition assays |
Isolated recombinant human protein was used for the HDAC1, 2, 4, 5, 6, 7, 8, 9, 10 and 11 assays, and HDAC3/NcoR2 complex was used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10 and 11 assays was a fluorogenic peptide from p53 residues 379 ~ 382 (RHKKAc); substrate for HDAC8 was fluorogenic diacyl peptide based on residues 379 ~ 382 of p53 (RHKAcKAc). Acetyl-Lys (trifluoroacetyl)-AMC substrate was used for HDAC4, 5, 7 and 9 assays. Tubastatin A was dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A was tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values were extracted by curve-fitting the dose/response slopes. |
| Cell experiment [2]: | |
|
Cell lines |
HaCaT cells |
|
Preparation method |
The solubility of this compound in DMSO is > 18.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
10 μM; 10 hrs |
|
Applications |
In HaCaT cells, Tubastatin A HCl selectively inhibited HDAC6, preventing sodium arsenite-induced association of Nrf2 mRNA with ribosomes and elevation of Nrf2 protein. |
| Animal experiment [3]: | |
|
Animal models |
B6/Rag1-/- mice adoptively transferred with 1 × 106 WT CD4+ CD45RBhi cells |
|
Dosage form |
25 mg/kg; i.p.; q.d., for 14 days |
|
Applications |
Adoptively transferred B6/Rag1-/- mice which were treated with Tubastatin A HCl recovered body weights and normal stool formation. In addition, the histologic examination showed reduced mononuclear cell infiltration, preservation of goblet cells, as well as intact mucosal surfaces. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Kyle V. Butler, Jay Kalin, Camille Brochier, et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A [J]. J. Am. Chem. Soc., 2010, 132 (31), pp 10842–10846. [2]. Kappeler KV, Zhang J, Dinh TN, et al. Histone deacetylase 6 associates with ribosomes and regulates de novo protein translation during arsenite stress [J]. Toxicol Sci. 2012 May;127(1):246-255. [3]. de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock WW. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May;31(10):2066-78. | |
| Cas No. | 1310693-92-5 | SDF | |
| Synonyms | TSA HCl;Tubastatin A hydrochloride | ||
| Chemical Name | N-hydroxy-4-[(2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)methyl]benzamide;hydrochloride | ||
| Canonical SMILES | CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl | ||
| Formula | C20H21N3O2.HCl | M.Wt | 371.86 |
| Solubility | ≥ 18.6mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *