Tubastatin A HCl

Catalog No.S2627

Tubastatin A HCl Chemical Structure

Molecular Weight(MW): 371.86

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).

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3 Customer Reviews

  • Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.

    Nat Commun 2014 5, 3479. Tubastatin A HCl purchased from Selleck.

    Tubastatin A gefitinib-induced apoptosis in NSCLC cells via activation of AKT. H358 cells were treated as described in Figure 4. Representative immunoblots of cleaved caspase-3, AKT and ERK1/2 and of their respective phosphorylated forms are shown. Actin was used as a protein-level control.

    Int J Cancer 2014 134(11):2560-71. Tubastatin A HCl purchased from Selleck.

  • GH cells were treated with 0.5 μM TSA or the DMSO solvent as indicated. Subsequently, Chromatin immunoprecipitation (ChIP) was performed with antibodies to NF-YB or a pre-immune control antibody. The DNA corresponding to the indicated promoters was quantified by real-time PCR and displayed in relation to the amount of input DNA. Bars indicate the standard error from three independent experiments.

    Oncotarget, 2016, 7(23):33484-97. Tubastatin A HCl purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

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

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 NFzTb5BMcW6jc3WgZZN{[Xl? NH[1fYwzNjVizszN NX3XXm4xTE2VTx?= NXv3SHRmcW6mdXPld{DPuS22dXL1cIlvKGi7cHXyZYNmfHmuYYTpc44> NXPTcY1vOjB4MUS5N|Y>
neuron cultures MV3GeY5kfGmxbjDhd5NigQ>? MnP2glExKM7:TR?= NXXQdYxZTE2VTx?= NHrmeXVxem:2ZXP0d{Bi\2GrboP0JIdtfXSjdHjpc45mKGSncHzleIlwdi2rbnT1Z4VlKG:6aXTheIl3\SC|dILld5M> MlnPNlA3OTR7M{[=
134/04 MkPsSpVv[3Srb36gZZN{[Xl? NGH1cG04NjViwsXN NVn1OJNJcW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> NWXPcI17OjJzN{S4N|k>
C2C12 NHfaW|RHfW6ldHnvckBie3OjeR?= NY\QfmNtPy53INM1US=> NXTRdXBOcW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> NYHKdWdCOjJzN{S4N|k>
HaCaT keratinocytes NFu3UplHfW6ldHnvckBie3OjeR?= NIXVTFQyOCEQvF2= Ml;5Zoxw[2u|IHHyd4VvcXSnIH\yc40hcW6mdXPpcochVnKoMjDwdo91\WmwIITyZY5{dGG2aX;u M3rrUVIzOzZ5Nki5
JURL-MK1 NVz3XJRjTnWwY4Tpc44h[XO|YYm= NVfu[IpQOTBizszN M33ze4VvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? M3TUUVI{ODJ{NUiz
CML-T1 MUnGeY5kfGmxbjDhd5NigQ>? NYnVNlkyOTBizszN MoXJ[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv M3jQXVI{ODJ{NUiz
K562 MVHGeY5kfGmxbjDhd5NigQ>? NYrTNoVuOTBizszN M1fFbIVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NWK1XIZTOjNyMkK1PFM>
HL-60 NGW5UHNHfW6ldHnvckBie3OjeR?= NYDhdZY6OTBizszN NXXVUlgy\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw NVzxcnF1OjNyMkK1PFM>
KMCH NV\BVXRoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUf2[HZ4hjFyIN88US=> NFK4[FBl\WO{ZXHz[ZMheHKxbHnm[ZJifGmxbjDhcoQh[W6laH;yZYdmNWmwZHXw[Y5l\W62IHfyc5d1cA>? MliyNlM{PzB|Mke=
THP-1 MX\GeY5kfGmxbjDhd5NigQ>? MYT+NVAh|ryP M4DMTIlvcGmkaYTzJHRPTi4QsTDhcoQhUUxvNjDz[YNz\XSrb36= MWqyN|U1OTZ|NB?=
RAW 264.7 Mn\VSpVv[3Srb36gZZN{[Xl? MnfSglExKM7:TR?= NWrpdVZW[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u MUeyN|U1OTZ|NB?=
HT3 MoLKSpVv[3Srb36gZZN{[Xl? NUnKdpBThjVizszN M3;XV2ROW09? NVLxflFscW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? MkH4NlM3QTh2Nki=
SiHa NFzBb5dHfW6ldHnvckBie3OjeR?= NHTWcHJ,PSEQvF2= MW\EUXNQ M33HeYlv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v MlvpNlM3QTh2Nki=
CaSki NI[yU2tHfW6ldHnvckBie3OjeR?= Mn3JglUh|ryP M1vB[mROW09? NYDDVVV1cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? MXqyN|Y6QDR4OB?=
SiHa MVzGeY5kfGmxbjDhd5NigQ>? NX7pW4tZhjVizszN MYLEUXNQ NH\mSYpqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> NFGwS3ozOzZ7OES2PC=>
CaSki Mo\xSpVv[3Srb36gZZN{[Xl? M1q3ZZ42KM7:TR?= NHvie|ZFVVOR MmC3bY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= NYjnZXdXOjN4OUi0Olg>
MCF-7 NXe3WnRsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHLsNWU{OCEQvF2= Ml\PSG1UVw>? MkHHTWM2OD1zNTFOwG0> MVGyN|c6QDZ6MB?=
MCF-7 MkPmSpVv[3Srb36gZZN{[Xl? NX:xTWk6OzBizszN NF\He|ZFVVOR NWXwepV{cW6lcnXhd4V{KHSqZTDtbYNzd3S3YoXs[UBi[2W2eXzheIlwdiCuZY\lcE4> NInQS28zOzd7OE[4NC=>
MCF-7 M17vb2Z2dmO2aX;uJIF{e2G7 Ml\YN|Ah|ryP NXjVW4F7TE2VTx?= NFXPNVZ{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IHPvcIQucW6mdXPl[EBl\XCxbInt[ZJqgmG2aX;u MVqyN|c6QDZ6MB?=
MCF-7 MXjGeY5kfGmxbjDhd5NigQ>? M1rMUVE2KM7:TR?= Mn3rSG1UVw>? NWr0V2k2e3SjYnnsbZpmeyCvaXPyc5R2[nWuZYOgZYdicW6|dDDuc4Nw\GG8b3zlMYlv\HWlZXSg[Il{[XO|ZX3icJk> NGnGPZAzOzd7OE[4NC=>
MCF-7 NX\KcnB3TnWwY4Tpc44h[XO|YYm= NF7YfVQ{OCEQvF2= NEnk[ndFVVOR MWjhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> NVntUHdnOjN5OUi2PFA>
MCF-7 M{DOV2Z2dmO2aX;uJIF{e2G7 NVmxUVBZOzBizszN M4ixNGROW09? MXfpcoNz\WG|ZYOgeIhmKGKrbnTpcochd2ZiSFTBR|Yhf2m2aDDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? MXGyN|c6QDZ6MB?=
PC12 M3u5ZmZ2dmO2aX;uJIF{e2G7 NGXnfId,OyEQvF2= MYXEUXNQ MVf1dE1z\We3bHH0[ZMh[W62aT3vfIll[XSrdnWg[4Vv\SCneIDy[ZN{cW:wIILlcIF1\WRidH:geJJidnOlcnnweIlwdiCoYXP0c5IhYEKSMYO= NHzDcYczPDlyOU[4Oi=>
PC12 NW\QNpY{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIftWZF,OyEQvF2= MVvEUXNQ NWm3eml7emW4ZYLz[UBJOk9{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NVn5So52OjR7MEm2PFY>
HEK293T NF7ZVZJHfW6ldHnvckBie3OjeR?= MlHyglMh|ryP MlvNSG1UVw>? Ml;veZAuemWpdXzheIVlKFiEUEHzJJBzd3SnaX6gcIV3\Wx? NILVSngzPDlyOU[4Oi=>
HEK293T MlLiSpVv[3Srb36gZZN{[Xl? NVvwVpl6hjNizszN NU\hbJd[TE2VTx?= NGjOUHNl\WyjeYOgXGJROXNicILveIVqdiCmZXfyZYRifGmxbjD2bYEh[WOndInsZZRqd25vbXXkbYF1\WRicILveIVie2:vYXyg[IVoemGmYYTpc44> M2T5dlI1QTB7Nki2
Huh7 MmHVSpVv[3Srb36gZZN{[Xl? NGTnRml,PSEQvF2= NHfl[VZFVVOR NVW0[3BYe3WycILld5NmeyCycn;sbYZmemG2aX;uJI9nKGincHH0bZRqeyCFII\pdpV{KHKncHzpZ49vKHerdHigSWM2OCB;IECuN{DPxE1? NETn[mYzPTFyOEOyOi=>
SKMEL21 M4HKNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVj+OVAxKG6P MXjEUXNQ MUXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MmTiNlU6PTd6MUK=
SKMEL103 NX7n[YpZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MoDjglUxOCCwTR?= NGjPVVJFVVOR NFnCbFRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M1HsUVI2QTV5OEGy
SKMEL28 MoSwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXn+OVAxKG6P M1;SZWROW09? MVHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NFvu[ZozPTl3N{ixNi=>
WM164 MUjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUfyTXA2hjVyMDDuUS=> Mmi5SG1UVw>? MVrpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NVXFclAzOjV7NUe4NVI>
WM1361a MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mn[3glUxOCCwTR?= NGTrc|lFVVOR M3rXN4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M2HkdlI2QTV5OEGy
WM1366 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVTaOmxOhjVyMDDuUS=> M2rVcWROW09? NXPa[INIcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NXO0flA4OjV7NUe4NVI>
WM793 MlXMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUSzPFdnhjVyMDDuUS=> NH;FOndFVVOR MV;pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M{PhTFI2QTV5OEGy
WM35 NIruRW9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXfSPW9ihjVyMDDuUS=> MUTEUXNQ NEe4NVZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NH3hXlAzPTl3N{ixNi=>
WM983a NXm1Vno5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4noXJ42ODBibl2= MXXEUXNQ MmjUbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MUKyOVk2PzhzMh?=
WM793 NFLHSVJHfW6ldHnvckBie3OjeR?= MoXGglYh|ryP M2D2V2ROW09? MWjpcoR2[2ViR{GgZZJz\XO2 M33CeVI2QTV5OEGy
WM164 MmX6SpVv[3Srb36gZZN{[Xl? Ml7mglYh|ryP MmfKSG1UVw>? MUXpcoR2[2ViR{GgZZJz\XO2 MUOyOVk2PzhzMh?=
WM983a NIj2PI1HfW6ldHnvckBie3OjeR?= MV3+OkDPxE1? MVjEUXNQ MWPpcoR2[2ViR{GgZZJz\XO2 M3frcVI2QTV5OEGy
WM164 NYDtbpZ1TnWwY4Tpc44h[XO|YYm= NWraO4NKhjNizszN NGDqVHlFVVOR NXi2ZpFk[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= MXGyOVk2PzhzMh?=
WM983a NIXxTohHfW6ldHnvckBie3OjeR?= NX7YWVN2hjNizszN NH76OYhFVVOR M3fZT4F2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? NXG3N|M{OjV7NUe4NVI>
IPC298 M1G3WmZ2dmO2aX;uJIF{e2G7 Mlf4glMh|ryP NEHu[WJFVVOR MlzNZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? MnH3NlU6PTd6MUK=
SKMEL30 MoKwSpVv[3Srb36gZZN{[Xl? MkTDglMh|ryP M4CwUGROW09? NGP3TnRifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| NVXWVHg{OjV7NUe4NVI>
TCa83 M4nzeWZ2dmO2aX;uJIF{e2G7 MX\pcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? MWiyOlI4QTNyMx?=
293T M4\q[mZ2dmO2aX;uJIF{e2G7 MonTglIh|rypL33s NYXrdYJ[cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NXHaOVF4OjZ{N{mzNFM>
SACC-83 NXzDSnd[TnWwY4Tpc44h[XO|YYm= M4jSXJ4zKM7:Zz;tcC=> NXG1N2tpcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= MV6yOlI4QTNyMx?=
293T NFPsToxHfW6ldHnvckBie3OjeR?= NWrwT4V2hjJizsznM41t M4jyd4lv\HWlZYOgVHRGViCjY3X0fYxifGmxbjDheEBMOTZ| MlSyNlYzPzl|MEO=
U-87 MG MUDGeY5kfGmxbjDhd5NigQ>? MljFglIh|rypL33s NYPhZVU4cW6qaXLpeJMhfGinIH3p[5JifGmxbjDhcoQhcW64YYPpc44> M4PDdVI3Ojd7M{Cz
U-87 MG NVTFXVFITnWwY4Tpc44h[XO|YYm= MoPKglExKM7:TR?= NUXEXXdKcW6qaXLpeJMhSUuWIIDoc5NxcG:{eXzheIlwdg>? NIHSeIEzPjJ5OUOwNy=>
U-87 MG M2HYcmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXP+NVAh|ryP MWHpcohq[mm2czDj[YxtKGe{b4f0bC=> MVmyOlI4QTNyMx?=

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Na?ve CD45RBhi CD4+ CD25- cells (1 × 106) from WT or HDAC6-/- mice Are injected i.p. into B6/Rag1-/-mice.
  • Formulation: Tubastatin A is dissolved in dimethyl sulfoxide (DMSO).
  • Dosages: 0.5 mg/kg
  • Administration: Tubastatin A is injected i.p. daily.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (198.99 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.86
Formula

C20H21N3O2.HCl

CAS No. 1310693-92-5
Storage powder
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID