Home Epigenetics HDAC inhibitor Tubastatin A HCl For research use only.

Tubastatin A HCl

Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).

Tubastatin A HCl Chemical Structure

Tubastatin A HCl Chemical Structure

CAS No. 1310693-92-5

Purity & Quality Control

Tubastatin A HCl Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
neuron cultures Kinase assay 2.5 μM DMSO induces α-tubulin hyperacetylation 20614936
neuron cultures Function assay ~10 μM DMSO protects against glutathione depletion-induced oxidative stress 20614936
134/04 Function assay 7.5 µM impairs myotube formation 22174839
C2C12 Function assay 7.5 µM impairs myotube formation 22174839
HaCaT keratinocytes Function assay 10 μM blocks arsenite from inducing Nrf2 protein translation 22367689
JURL-MK1 Function assay 10 μM enhances cell adhesivity to fibronectin 23022583
CML-T1 Function assay 10 μM enhances cell adhesivity to fibronectin 23022583
K562 Function assay 10 μM enhances cell adhesivity to fibronectin 23022583
HL-60 Function assay 10 μM enhances cell adhesivity to fibronectin 23022583
KMCH Growth inhibitory assay ~10 μM decreases proliferation and anchorage-independent growth 23370327
THP-1 Function assay ~10 μM inhibits TNF-α and IL-6 secretion 23541634
RAW 264.7 Function assay ~10 μM attenuates NO production 23541634
HT3 Function assay ~5 μM DMSO induces the differential α-tubulin acetylation 23698468
SiHa Function assay ~5 μM DMSO induces the differential α-tubulin acetylation 23698468
CaSki Function assay ~5 μM DMSO induces the differential α-tubulin acetylation 23698468
SiHa Function assay ~5 μM DMSO inhibits Thapsigargin- or EGF-induced SOCE activation 23698468
CaSki Function assay ~5 μM DMSO inhibits Thapsigargin- or EGF-induced SOCE activation 23698468
MCF-7 Growth inhibitory assay 30 μM DMSO IC50=15 μM 23798680
MCF-7 Function assay 30 μM DMSO increases the microtubule acetylation level. 23798680
MCF-7 Function assay 30 μM DMSO stabilizes microtubules against cold-induced depolymerization 23798680
MCF-7 Function assay 15 μM DMSO stabilizes microtubules against nocodazole-induced disassembly 23798680
MCF-7 Function assay 30 μM DMSO alteres the assembly dynamics of interphase microtubules 23798680
MCF-7 Function assay 30 μM DMSO increases the binding of HDAC6 with interphase microtubules 23798680
PC12 Function assay ~3 μM DMSO up-regulates anti-oxidative gene expression related to transcription factor XBP1s 24909686
PC12 Growth inhibitory assay ~3 μM DMSO reverse H2O2-induced growth inhibition 24909686
HEK293T Function assay ~3 μM DMSO up-regulated XBP1s protein level 24909686
HEK293T Function assay ~3 μM DMSO delays XBP1s protein degradation via acetylation-mediated proteasomal degradation 24909686
Huh7 Function assay ~5 μM DMSO suppresses proliferation of hepatitis C virus replicon with EC50 = 0.3 μM 25108326
SKMEL21 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
SKMEL103 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
SKMEL28 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM164 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM1361a Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM1366 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM793 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM35 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM983a Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation 25957812
WM793 Function assay ~6 μM DMSO induce G1 arrest 25957812
WM164 Function assay ~6 μM DMSO induce G1 arrest 25957812
WM983a Function assay ~6 μM DMSO induce G1 arrest 25957812
WM164 Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens 25957812
WM983a Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens 25957812
IPC298 Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens 25957812
SKMEL30 Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens 25957812
TCa83 Function assay induces PTEN expression and membrane translocation 26279303
293T Function assay ~2 μg/ml induces PTEN expression and membrane translocation 26279303
SACC-83 Function assay ~2 μg/ml induces PTEN expression and membrane translocation 26279303
293T Function assay ~2 μg/ml induces PTEN acetylation at K163 26279303
U-87 MG Function assay ~2 μg/ml inhibits the migration and invasion 26279303
U-87 MG Function assay ~10 μM inhibits AKT phosphorylation 26279303
U-87 MG Growth inhibitory assay ~10 μM inhibits cell growth 26279303
Click to View More Cell Line Experimental Data

Biological Activity

Description Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
Targets
HDAC6 [1]
(Cell-free assay)		 HDAC8 [1]
(Cell-free assay)
15 nM 854 nM
In vitro
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 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. [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]
Kinase Assay Enzyme Inhibition Assays
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.
Cell Research Cell lines Primary cortical neuron of fetal Sprague-Dawley rats (embryonic day 17)
Concentrations 0-10 μM
Incubation Time 24 hours
Method Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. 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 (Invitrogen) 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot EGFR / p-AKT / AKT / p-ERK / ERK 29665050
Immunofluorescence α-tubulin / Acetylated tubulin HDAC6 23798680
In Vivo
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. [2]
Animal Research Animal Models Na?ve CD45RBhi CD4+ CD25- cells (1 × 106) from WT or HDAC6-/- mice Are injected i.p. into B6/Rag1-/-mice.
Dosages 0.5 mg/kg
Administration Tubastatin A is injected i.p. daily.

Chemical Information & Solubility

Molecular Weight 371.86 Formula

C20H21N3O2.HCl
CAS No. 1310693-92-5 SDF Download Tubastatin A HCl SDF
Smiles CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (268.91 mM) Warmed with 50°C water bath; Ultrasonicated; Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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