Tubastatin A Hydrochloride (Synonyms: Tubastatin A HCl; TSA HCl)

Name: Tubastatin A Hydrochloride
Brand: MedChemExpress
SKU: HY-13271
Rating: 5.0 (28 reviews)

Cat. No.: HY-13271 Purity: 98.19%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC₅₀ of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

For research use only. We do not sell to patients.

Tubastatin A Hydrochloride Chemical Structure

CAS No. : 1310693-92-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of Tubastatin A Hydrochloride:

Tubastatin A In-stock
Tubastatin A TFA Get quote

24 Publications Citing Use of MCE Tubastatin A Hydrochloride

RT-PCR

: Tubastatin A Hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Oct 21;13(10):888. [Abstract]; Construction of HCT116 cell line with stable HDAC6 knockdown. Tubastatin A HCl is HDAC6 selective inhibitor.

: Tubastatin A Hydrochloride purchased from MedChemExpress. Usage Cited in: J Nutr. 2020 Jul 1;150(7):1790-1798. [Abstract]; Effects of TBSA (Tubastatin A) pretreatment on glucose-induced changes in mRNA amounts of genes in IECs of yellow catfish.

: Tubastatin A Hydrochloride purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Feb 1;9:34. [Abstract]; HDAC6 inhibition with Tubastatin A acetylates TFEB, facilitates TFEB nuclear translocation and attenuates programmed cell death in NRK-52E cells. Immunoblotting for acetylated α-tubulin in NRK-52E cells treated with Tubastatin A.

: Tubastatin A Hydrochloride purchased from MedChemExpress. Usage Cited in: Medical Science, University of Toronto. 2017 Nov.; Tubastatin A induces a dose-dependent increase in acetylated α-tubulin levels in NRK-52E cells.

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Metallo-β-lactamase

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HDAC6

15 nM (IC₅₀)

HDAC8

854 nM (IC₅₀)

HDAC1

16400 nM (IC₅₀)

In Vitro

Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM^[1]. At 100 ng/mL Tubastatin A increases Foxp³⁺ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro^[2]. Tubastatin A treatment in CC12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes^[3]. A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Daily treatment of Tubastatin A at 0.5 mg/kg inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

371.86

Formula

C₂₀H₂₂ClN₃O₂

CAS No.

1310693-92-5

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC=C(C=C1)CN2C3=C(C4=C2C=CC=C4)CN(C)CC3)NO.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 10.8 mg/mL (29.04 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 6.67 mg/mL (17.94 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.62 mg/mL (7.05 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.62 mg/mL (7.05 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.52 mg/mL (1.40 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.19%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (254 KB) LCMS (259 KB)

Handling Instructions (2659 KB)

References

[1]. Kyle V. Butler et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A J. Am. Chem. Soc., 2010, 132 (31), pp 10842-10846 [Content Brief]

[2]. de Zoeten EF, et al. 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. [Content Brief]

[3]. Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563 [Content Brief]

[4]. Ketene AN, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells. Integr Biol (Camb). 2012 May;4(5):540-9. [Content Brief]

[5]. Brijmohan AS, et al. HDAC6 Inhibition Promotes Transcription Factor EB Activation and Is Protective in Experimental Kidney Disease. Front Pharmacol. 2018 Feb 1;9:34. [Content Brief]

[6]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. [Content Brief]

Kinase Assay ^[1]	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 use 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. Tubastatin A is 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17). All experiments are initiated 24 hours after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells are rinsed with warm PBS and then placed in minimum essential medium containing 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress is induced by the addition of the glutamate analogue homocysteate (HCA; 5 mM) to the media. HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. In combination with HCA, neurons are treated with Tubastatin A at the indicated concentrations. Viability is assessed after 24 hours by MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	The effects of HDAC6 targeting in dextran sodium sulfate (DSS) and adoptive transfer models of colitis are evaluated, using 10 mice per group. Freshly prepared 4% (wt/vol) DSS is added daily for 5 days to the pH-balanced tap water of WT B6 mice. Mice are treated daily for 7 days with tubacin or niltubacin (0.5 mg/kg of body weight/day, i.p.), and colitis is assessed by daily monitoring of body weight, stool consistency, and fecal blood. Stool consistency is scored as 0 (hard), 2 (soft), or 4 (diarrhea), and fecal blood (Hemoccult) is scored as 0 (absent), 2 (occult), or 4 (gross). To assess prevention of colitis in a T cell-dependent model, CD⁴⁺ CD45RBhi T cells (1×10⁶) isolated from WT mice using magnetic beads (>95% cell purity, flow cytometry) are injected i.p. into B6/Rag1^−/− mice plus CD⁴⁺ CD²⁵⁺ Tregs (1.25×10⁵) isolated using magnetic beads from HDAC6^−/− or WT mice (>90% Treg purity, flow cytometry) and mice are monitored biweekly for clinical evidence of colitis. To assess therapy of established T cell-dependent colitis, B6/Rag1^−/− mice are injected i.p. with CD⁴⁺ CD45RBhi cells (1×10⁶). Once colitis has developed, mice also receive CD⁴⁺ CD²⁵⁺ Tregs (5×10⁵ cells) isolated as described above from HDAC6^−/− or WT mice or treatment with HDAC6i (tubastatin A) or HSP90i (17-AAG). Mice are monitored for continued weight loss and stool consistency. At the cessation of the study, paraffin sections of colons stained with Alcian Blue or hematoxylin and eosin are graded histologically or evaluated by immunoperoxidase staining for Foxp³⁺ Treg infiltration. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Kyle V. Butler et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A J. Am. Chem. Soc., 2010, 132 (31), pp 10842-10846 [Content Brief] [2]. de Zoeten EF, et al. 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. [Content Brief] [3]. Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563 [Content Brief] [4]. Ketene AN, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells. Integr Biol (Camb). 2012 May;4(5):540-9. [Content Brief] [5]. Brijmohan AS, et al. HDAC6 Inhibition Promotes Transcription Factor EB Activation and Is Protective in Experimental Kidney Disease. Front Pharmacol. 2018 Feb 1;9:34. [Content Brief] [6]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.6892 mL	13.4459 mL	26.8918 mL	67.2296 mL
	5 mM	0.5378 mL	2.6892 mL	5.3784 mL	13.4459 mL
	10 mM	0.2689 mL	1.3446 mL	2.6892 mL	6.7230 mL
	15 mM	0.1793 mL	0.8964 mL	1.7928 mL	4.4820 mL
DMSO	20 mM	0.1345 mL	0.6723 mL	1.3446 mL	3.3615 mL
DMSO	25 mM	0.1076 mL	0.5378 mL	1.0757 mL	2.6892 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Tubastatin A Hydrochloride Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tubastatin A1310693-92-5Tubastatin A HCl TSA HClBeta-lactamaseHDACAutophagyApoptosisβ-lactamaseHistone deacetylasesInhibitorinhibitorinhibit

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Tubastatin A Hydrochloride (Synonyms: Tubastatin A HCl; TSA HCl)

Customer Review

Other Forms of Tubastatin A Hydrochloride:

Tubastatin A Hydrochloride Related Antibodies

24 Publications Citing Use of MCE Tubastatin A Hydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Beta-lactamase Isoform Specific Products:

View All HDAC Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Tubastatin A Hydrochloride Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Tubastatin A Hydrochloride Related Classifications

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