Tubastatin A HCl

Catalog No.S2627 Synonyms: TSA HCl

For research use only.

Tubastatin A HCl (TSA) 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

CAS No. 1310693-92-5

Selleck's Tubastatin A HCl has been cited by 43 publications

Purity & Quality Control

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Biological Activity

Description Tubastatin A HCl (TSA) 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
neuron cultures NF;pSphMcW6jc3WgZZN{[Xl? Ml3uNk42KM7:TR?= MYrEUXNQ MYrpcoR2[2W|IN8xMZR2[nWuaX6gbJlx\XKjY3X0fYxifGmxbh?= M3;aVVIxPjF2OUO2
neuron cultures NGXPSphHfW6ldHnvckBie3OjeR?= MlHLglExKM7:TR?= MWDEUXNQ MXPwdo91\WO2czDh[4FqdnO2IHfseZRifGirb37lJIRmeGyndHnvck1qdmS3Y3XkJI95cWSjdHn2[UB{fHKnc4O= NUfBV3NjOjB4MUS5N|Y>
134/04 MlvJSpVv[3Srb36gZZN{[Xl? NYjWfZc6Py53INM1US=> NXTYXJVScW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> NGewWYgzOjF5NEizPS=>
C2C12 NEjmWoZHfW6ldHnvckBie3OjeR?= NXex[ZZQPy53INM1US=> M3TlOolueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= M2ThSFIzOTd2OEO5
HaCaT keratinocytes M3zNN2Z2dmO2aX;uJIF{e2G7 NHj6XGwyOCEQvF2= NGr1bYRjdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> MXSyNlM3PzZ6OR?=
JURL-MK1 M3HDOWZ2dmO2aX;uJIF{e2G7 Mlr2NVAh|ryP MWDlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MkT3NlMxOjJ3OEO=
CML-T1 M{TaWmZ2dmO2aX;uJIF{e2G7 NHTiWIsyOCEQvF2= MlT1[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv NWDRfoVvOjNyMkK1PFM>
K562 MXTGeY5kfGmxbjDhd5NigQ>? MlrhNVAh|ryP M3rGcoVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NFvaXI8zOzB{MkW4Ny=>
HL-60 NXvPfGlOTnWwY4Tpc44h[XO|YYm= MnXyNVAh|ryP MULlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> NUnOTY81OjNyMkK1PFM>
KMCH MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml6yglExKM7:TR?= Ml[2[IVkemWjc3XzJJBzd2yrZnXyZZRqd25iYX7kJIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIg> NUjLRmEyOjN|N{CzNlc>
THP-1 MkLmSpVv[3Srb36gZZN{[Xl? NIe0XYl,OTBizszN NIXYUGxqdmirYnn0d{BVVkZvzsGgZY5lKEmOLU[gd4VkemW2aX;u M1TGclI{PTRzNkO0
RAW 264.7 MoXvSpVv[3Srb36gZZN{[Xl? MUT+NVAh|ryP NY\ZWpM6[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u MlzUNlM2PDF4M{S=
HT3 NYfVV|dRTnWwY4Tpc44h[XO|YYm= M{DUdJ42KM7:TR?= NXOye3N6TE2VTx?= M4LLdolv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v NWPESYdKOjN4OUi0Olg>
SiHa MmL4SpVv[3Srb36gZZN{[Xl? NVv4SGFPhjVizszN NGT0OY5FVVOR NG\VZ|VqdmS3Y3XzJJRp\SCmaX\m[ZJmdnSrYXyg{tEufHWkdXzpckBi[2W2eXzheIlwdg>? M2rNXlI{Pjl6NE[4
CaSki M2TvfWZ2dmO2aX;uJIF{e2G7 NVT6[|ZshjVizszN MoXHSG1UVw>? MXLpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> MlzKNlM3QTh2Nki=
SiHa M{fN[GZ2dmO2aX;uJIF{e2G7 NFrSXZF,PSEQvF2= NWnKSoJWTE2VTx?= MVfpcohq[mm2czDUbIFxe2mpYYLnbY4uKG:{IFXHSk1qdmS3Y3XkJHNQS0ViYXP0bZZifGmxbh?= NXnmOmx5OjN4OUi0Olg>
CaSki MY\GeY5kfGmxbjDhd5NigQ>? Ml;5glUh|ryP NYW3T3k2TE2VTx?= MVjpcohq[mm2czDUbIFxe2mpYYLnbY4uKG:{IFXHSk1qdmS3Y3XkJHNQS0ViYXP0bZZifGmxbh?= M36zfVI{Pjl6NE[4
MCF-7 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEHxO|Q{OCEQvF2= NXrrZYpyTE2VTx?= MnHWTWM2OD1zNTFOwG0> MUSyN|c6QDZ6MB?=
MCF-7 MnzGSpVv[3Srb36gZZN{[Xl? M17tcFMxKM7:TR?= NUH1THp6TE2VTx?= MV;pcoNz\WG|ZYOgeIhmKG2rY4LveJVjfWynIHHj[ZR6dGG2aX;uJIxmfmWuLh?= MnjrNlM4QTh4OEC=
MCF-7 MlXJSpVv[3Srb36gZZN{[Xl? MVKzNEDPxE1? NUjjdWxlTE2VTx?= MVPzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KGOxbHStbY5lfWOnZDDk[ZBwdHmvZYLpfoF1cW:w MW[yN|c6QDZ6MB?=
MCF-7 NXuwTW0{TnWwY4Tpc44h[XO|YYm= M4XDUFE2KM7:TR?= M{TjPGROW09? NF7wd|d{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IH7vZ49l[XqxbHWtbY5lfWOnZDDkbZNie3OnbXLsfS=> MVWyN|c6QDZ6MB?=
MCF-7 MYfGeY5kfGmxbjDhd5NigQ>? NYLEd5ptOzBizszN NVPEXoRuTE2VTx?= NETDPGtidHSncnXzJJRp\SCjc4PlcYJtgSCmeX7hcYlkeyCxZjDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? M2m2WlI{Pzl6Nkiw
MCF-7 NEnqcZpHfW6ldHnvckBie3OjeR?= M1nhRVMxKM7:TR?= M3XIcWROW09? NVjFfXF5cW6lcnXhd4V{KHSqZTDibY5lcW6pIH;mJGhFSUN4IIfpeIghcW62ZYLwbIF{\SCvaXPyc5R2[nWuZYO= M4f5PVI{Pzl6Nkiw
PC12 NGnGV|ZHfW6ldHnvckBie3OjeR?= MX\+N{DPxE1? NYPCeZE6TE2VTx?= MkX1eZAuemWpdXzheIV{KGGwdHmtc5hq\GG2aY\lJIdmdmViZYjwdoV{e2mxbjDy[YxifGWmIITvJJRz[W6|Y4LpdJRqd25iZnHjeI9zKFiEUEHz NH60XVczPDlyOU[4Oi=>
PC12 M4fa[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXSycFhrhjNizszN NX\R[lA3TE2VTx?= NVryTWQ4emW4ZYLz[UBJOk9{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NVnFRpc4OjR7MEm2PFY>
HEK293T NYK5bHdWTnWwY4Tpc44h[XO|YYm= M3;uNJ4{KM7:TR?= MWXEUXNQ NUTmWlFJfXBvcnXneYxifGWmIGjCVFF{KHC{b4TlbY4hdGW4ZXy= MmLUNlQ6ODl4OE[=
HEK293T NVrDZYVqTnWwY4Tpc44h[XO|YYm= MojZglMh|ryP M17KS2ROW09? Mmfq[IVt[Xm|IGjCVFF{KHC{b4TlbY4h\GWpcnHkZZRqd25idnnhJIFk\XS7bHH0bY9vNW2nZHnheIVlKHC{b4TlZZNwdWGuIHTl[5Ji\GG2aX;u NXryeYh4OjR7MEm2PFY>
Huh7 NG\CfodHfW6ldHnvckBie3OjeR?= NY\wWnF5hjVizszN MVnEUXNQ NWf1cJRbe3WycILld5NmeyCycn;sbYZmemG2aX;uJI9nKGincHH0bZRqeyCFII\pdpV{KHKncHzpZ49vKHerdHigSWM2OCB;IECuN{DPxE1? NEnBNoUzPTFyOEOyOi=>
SKMEL21 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYDXeVNvhjVyMDDuUS=> MV3EUXNQ MUnpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NWj3clF3OjV7NUe4NVI>
SKMEL103 NF[yc3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2DjUp42ODBibl2= NIXiV5hFVVOR MWXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M17TUFI2QTV5OEGy
SKMEL28 NV[0fYhmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MljxglUxOCCwTR?= M2WydGROW09? MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NYK5dJdxOjV7NUe4NVI>
WM164 M4jnW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlTxglUxOCCwTR?= NHrnZ2RFVVOR NULlfY1zcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NVXKWJFMOjV7NUe4NVI>
WM1361a NUXZ[nFQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlTIglUxOCCwTR?= MWHEUXNQ M3yyUIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MlvlNlU6PTd6MUK=
WM1366 M{[4cWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFm2c3N,PTByIH7N MlHhSG1UVw>? NY[3ZlJ{cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MVmyOVk2PzhzMh?=
WM793 NX\4S3BST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MonrglUxOCCwTR?= M{DCWWROW09? M4n6VIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NF7NZYUzPTl3N{ixNi=>
WM35 M{DZfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn33glUxOCCwTR?= MYXEUXNQ Mo\wbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M1XJPVI2QTV5OEGy
WM983a NVnPOG12T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXjFPIhHhjVyMDDuUS=> NF\1cmxFVVOR NFmwN21qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NXT1R21OOjV7NUe4NVI>
WM793 MnfSSpVv[3Srb36gZZN{[Xl? MkP5glYh|ryP MXTEUXNQ NFy3V2RqdmS3Y3WgS|Eh[XK{ZYP0 M{DRd|I2QTV5OEGy
WM164 M3fL[GZ2dmO2aX;uJIF{e2G7 NU\yNpBHhjZizszN MoH0SG1UVw>? MYXpcoR2[2ViR{GgZZJz\XO2 M{nKfFI2QTV5OEGy
WM983a M3z4NWZ2dmO2aX;uJIF{e2G7 M2XPTp43KM7:TR?= NWrFUJBZTE2VTx?= MoP6bY5lfWOnIFexJIFzemW|dB?= M1XWN|I2QTV5OEGy
WM164 M1HmTWZ2dmO2aX;uJIF{e2G7 NUfjdlVshjNizszN MXLEUXNQ M4n5PIF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? NXixU2M1OjV7NUe4NVI>
WM983a NGfOPW1HfW6ldHnvckBie3OjeR?= MmnDglMh|ryP M2rDSGROW09? NXfOelZx[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= M1LPV|I2QTV5OEGy
IPC298 NGHoZ2tHfW6ldHnvckBie3OjeR?= NYri[GZ[hjNizszN NXnkfXpHTE2VTx?= MY\heYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ M1XwbFI2QTV5OEGy
SKMEL30 NVrRUY5ZTnWwY4Tpc44h[XO|YYm= NYPzW25JhjNizszN NWWzdYhwTE2VTx?= NX\LT|hS[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= MoDRNlU6PTd6MUK=
TCa83 MoLVSpVv[3Srb36gZZN{[Xl? NWjRTllwcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= Mkj3NlYzPzl|MEO=
293T M2fQbGZ2dmO2aX;uJIF{e2G7 NEnGUld,OiEQvHevcYw> M1rKZolv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NETMfnYzPjJ5OUOwNy=>
SACC-83 M1zXOGZ2dmO2aX;uJIF{e2G7 NY\TW|lQhjJizsznM41t NWX0NZMycW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NGj2TVczPjJ5OUOwNy=>
293T MVfGeY5kfGmxbjDhd5NigQ>? MoftglIh|rypL33s MW\pcoR2[2W|IGDUSW4h[WOndInsZZRqd25iYYSgT|E3Ow>? NX7NPWk1OjZ{N{mzNFM>
U-87 MG M{izOWZ2dmO2aX;uJIF{e2G7 NH\zOIx,OiEQvHevcYw> NW\6WFhncW6qaXLpeJMhfGinIH3p[5JifGmxbjDhcoQhcW64YYPpc44> MlnBNlYzPzl|MEO=
U-87 MG Mlf0SpVv[3Srb36gZZN{[Xl? NVWwZ4E{hjFyIN88US=> NHHGT25qdmirYnn0d{BCU1RicHjvd5Bpd3K7bHH0bY9v NXf4fIlQOjZ{N{mzNFM>
U-87 MG NFvScoxIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{O2b54yOCEQvF2= NGTGUFlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4fleFI3Ojd7M{Cz
Assay
Methods Test Index PMID
Western blot EGFR / p-AKT / AKT / p-ERK / ERK 29665050
Immunofluorescence α-tubulin / Acetylated tubulin ; HDAC6 23798680
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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:[1]
  • 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.
Animal Research:[2]
  • 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.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.

1 mg/mL

Chemical Information

Molecular Weight 371.86
Formula

C20H21N3O2.HCl

CAS No. 1310693-92-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl

In vivo Formulation Calculator (Clear solution)

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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.
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Tech Support

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