Name: Tubastatin A HCl
Brand: Selleck Chemicals
SKU: S2627
Availability: InStock
Rating: 5 (47 reviews)

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Quality Control

Batch: Purity: 99.30%

99.30

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Inhibitors	Entinostat (MS-275) RGFP966 Tubastatin A Fimepinostat (CUDC-907) Trichostatin A (TSA) Mocetinostat (MGCD0103) Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) Dihydrochloride MC1568 PCI-34051

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Formulation	Activity Description
neuron cultures	Kinase assay	2.5 μM	DMSO	induces α-tubulin hyperacetylation
neuron cultures	Function assay	~10 μM	DMSO	protects against glutathione depletion-induced oxidative stress
134/04	Function assay	7.5 µM		impairs myotube formation
C2C12	Function assay	7.5 µM		impairs myotube formation
HaCaT keratinocytes	Function assay	10 μM		blocks arsenite from inducing Nrf2 protein translation
JURL-MK1	Function assay	10 μM		enhances cell adhesivity to fibronectin
CML-T1	Function assay	10 μM		enhances cell adhesivity to fibronectin
K562	Function assay	10 μM		enhances cell adhesivity to fibronectin
HL-60	Function assay	10 μM		enhances cell adhesivity to fibronectin
KMCH	Growth inhibitory assay	~10 μM		decreases proliferation and anchorage-independent growth
THP-1	Function assay	~10 μM		inhibits TNF-α and IL-6 secretion
RAW 264.7	Function assay	~10 μM		attenuates NO production
HT3	Function assay	~5 μM	DMSO	induces the differential α-tubulin acetylation
SiHa	Function assay	~5 μM	DMSO	induces the differential α-tubulin acetylation
CaSki	Function assay	~5 μM	DMSO	induces the differential α-tubulin acetylation
SiHa	Function assay	~5 μM	DMSO	inhibits Thapsigargin- or EGF-induced SOCE activation
CaSki	Function assay	~5 μM	DMSO	inhibits Thapsigargin- or EGF-induced SOCE activation
MCF-7	Growth inhibitory assay	30 μM	DMSO	IC50=15 μM
MCF-7	Function assay	30 μM	DMSO	increases the microtubule acetylation level.
MCF-7	Function assay	30 μM	DMSO	stabilizes microtubules against cold-induced depolymerization
MCF-7	Function assay	15 μM	DMSO	stabilizes microtubules against nocodazole-induced disassembly
MCF-7	Function assay	30 μM	DMSO	alteres the assembly dynamics of interphase microtubules
MCF-7	Function assay	30 μM	DMSO	increases the binding of HDAC6 with interphase microtubules
PC12	Function assay	~3 μM	DMSO	up-regulates anti-oxidative gene expression related to transcription factor XBP1s
PC12	Growth inhibitory assay	~3 μM	DMSO	reverse H2O2-induced growth inhibition
HEK293T	Function assay	~3 μM	DMSO	up-regulated XBP1s protein level
HEK293T	Function assay	~3 μM	DMSO	delays XBP1s protein degradation via acetylation-mediated proteasomal degradation
Huh7	Function assay	~5 μM	DMSO	suppresses proliferation of hepatitis C virus replicon with EC50 = 0.3 μM
SKMEL21	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
SKMEL103	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
SKMEL28	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM164	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM1361a	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM1366	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM793	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM35	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM983a	Growth inhibitory assay	~500 nM	DMSO	inhibits cell proliferation
WM793	Function assay	~6 μM	DMSO	induce G1 arrest
WM164	Function assay	~6 μM	DMSO	induce G1 arrest
WM983a	Function assay	~6 μM	DMSO	induce G1 arrest
WM164	Function assay	~3 μM	DMSO	augments expression of MHC class I and melanoma associated antigens
WM983a	Function assay	~3 μM	DMSO	augments expression of MHC class I and melanoma associated antigens
IPC298	Function assay	~3 μM	DMSO	augments expression of MHC class I and melanoma associated antigens
SKMEL30	Function assay	~3 μM	DMSO	augments expression of MHC class I and melanoma associated antigens
TCa83	Function assay			induces PTEN expression and membrane translocation
293T	Function assay	~2 μg/ml		induces PTEN expression and membrane translocation
SACC-83	Function assay	~2 μg/ml		induces PTEN expression and membrane translocation
293T	Function assay	~2 μg/ml		induces PTEN acetylation at K163
U-87 MG	Function assay	~2 μg/ml		inhibits the migration and invasion
U-87 MG	Function assay	~10 μM		inhibits AKT phosphorylation
U-87 MG	Growth inhibitory assay	~10 μM		inhibits cell growth
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (268.91 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (13.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.69mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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.

Chemical Information, Storage & Stability

Molecular Weight	371.86	Formula	C₂₀H₂₁N₃O₂.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1310693-92-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	HDAC6 (Cell-free assay) 15 nM HDAC8 (Cell-free assay) 854 nM
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. At 100 ng/mL Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro. Tubastatin A treatment in C2C12 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. 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.
Kinase Assay	Enzyme Inhibition Assays
Kinase Assay	Enzyme inhibition assays are performed by the Reaction Biology Corporation, Malvern, PA, using the Reaction Biology HDAC Spectrum platform. (www.reactionbiology.com) 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.
In vivo	Daily treatment of Tubastatin A at 0.5mg/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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20614936/ [2] https://pubmed.ncbi.nlm.nih.gov/21444725/ [3] https://pubmed.ncbi.nlm.nih.gov/22174839/ [4] https://pubmed.ncbi.nlm.nih.gov/22446682/

Applications

Methods	Biomarkers	Images	PMID
Western blot	EGFR / p-AKT / AKT / p-ERK / ERK		29665050
Immunofluorescence	α-tubulin / Acetylated tubulin HDAC6		23798680

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Tubastatin A HCl HDAC inhibitor

Chemical Structure

Molecular Weight: 371.86