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 MXrLbY5ie2ViYYPzZZk> MX:yMlUh|ryP MYjEUXNQ Ml\0bY5lfWOnczFOtU11fWK3bHnuJIh6eGW{YXPleJlt[XSrb36= MYeyNFYyPDl|Nh?=
neuron cultures NV3qe2hVTnWwY4Tpc44h[XO|YYm= NEDNdll,OTBizszN NVHtSndMTE2VTx?= MoPGdJJwfGWldIOgZYdicW6|dDDncJV1[XSqaX;u[UBl\XCuZYTpc44ucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz MmnKNlA3OTR7M{[=
134/04 MlPOSpVv[3Srb36gZZN{[Xl? Mn20O{42KML3TR?= NUnGZ|dJcW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> NV7FfXp7OjJzN{S4N|k>
C2C12 M3n4cGZ2dmO2aX;uJIF{e2G7 M1zrdVcvPSEEtV2= M4iyOolueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= M2fUXVIzOTd2OEO5
HaCaT keratinocytes MnPhSpVv[3Srb36gZZN{[Xl? NV\S[ng{OTBizszN M4n2boJtd2OtczDhdpNmdmm2ZTDmdo9uKGmwZIXjbY5oKE6{ZkKgdJJwfGWrbjD0doFve2yjdHnvci=> M3PSRlIzOzZ5Nki5
JURL-MK1 NWjMS3JmTnWwY4Tpc44h[XO|YYm= NYDleWI6OTBizszN NILKUVNmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MlHqNlMxOjJ3OEO=
CML-T1 NH;T[olHfW6ldHnvckBie3OjeR?= MW[xNEDPxE1? NEfYeIJmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? M3:3[VI{ODJ{NUiz
K562 M4TDWGZ2dmO2aX;uJIF{e2G7 MWKxNEDPxE1? MXTlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> NGDSOI0zOzB{MkW4Ny=>
HL-60 MWDGeY5kfGmxbjDhd5NigQ>? MUixNEDPxE1? NVG0cVlv\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw NX7le3RiOjNyMkK1PFM>
KMCH MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUX+NVAh|ryP MUDk[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> NYqxfGJLOjN|N{CzNlc>
THP-1 NXrwSJpKTnWwY4Tpc44h[XO|YYm= M2fEep4yOCEQvF2= M3rVWIlvcGmkaYTzJHRPTi4QsTDhcoQhUUxvNjDz[YNz\XSrb36= NV3lNnVKOjN3NEG2N|Q>
RAW 264.7 M2PPTGZ2dmO2aX;uJIF{e2G7 MXf+NVAh|ryP M4jlVYF1fGWwdXH0[ZMhVk9icILv[JVkfGmxbh?= MWeyN|U1OTZ|NB?=
HT3 M1fDRmZ2dmO2aX;uJIF{e2G7 NVv1UolvhjVizszN NWXFdYFGTE2VTx?= MoHJbY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> NFjNbWYzOzZ7OES2PC=>
SiHa NEDLU3NHfW6ldHnvckBie3OjeR?= NITkRnN,PSEQvF2= MYPEUXNQ NWrWeWxCcW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? NHHkfFkzOzZ7OES2PC=>
CaSki NEHVcGhHfW6ldHnvckBie3OjeR?= M1PzXp42KM7:TR?= MWLEUXNQ M4r0e4lv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v NX3pZo5SOjN4OUi0Olg>
SiHa NI\jZVVHfW6ldHnvckBie3OjeR?= NFXUenl,PSEQvF2= MVfEUXNQ MorhbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= NGO3O4EzOzZ7OES2PC=>
CaSki MU\GeY5kfGmxbjDhd5NigQ>? MXL+OUDPxE1? NEP1PFdFVVOR NWK5NVFvcW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> NWjPOYlqOjN4OUi0Olg>
MCF-7 NGTWblNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUGzNEDPxE1? NEW1eG9FVVOR NGW3T|NKSzVyPUG1JO69VQ>? MYWyN|c6QDZ6MB?=
MCF-7 MnPhSpVv[3Srb36gZZN{[Xl? NETxSFQ{OCEQvF2= NUL6dmJbTE2VTx?= NFqxZYJqdmO{ZXHz[ZMhfGinIH3pZ5JwfHWkdXzlJIFk\XS7bHH0bY9vKGyndnXsMi=> MWWyN|c6QDZ6MB?=
MCF-7 Mnf6SpVv[3Srb36gZZN{[Xl? NYO3cpdFOzBizszN NGTZV4dFVVOR MmHQd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCClb3zkMYlv\HWlZXSg[IVxd2y7bXXybZpifGmxbh?= M3\mUFI{Pzl6Nkiw
MCF-7 NXn2VJExTnWwY4Tpc44h[XO|YYm= MV6xOUDPxE1? NXnuS3h[TE2VTx?= Ml;Zd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCCwb3Pv[IF7d2ynLXnu[JVk\WRiZHnzZZN{\W2kbIm= M{naTlI{Pzl6Nkiw
MCF-7 M{jlNmZ2dmO2aX;uJIF{e2G7 MXOzNEDPxE1? NFO5ZZhFVVOR MlPiZYx1\XKnczD0bIUh[XO|ZX3icJkh\HmwYX3pZ5Mhd2ZiaX70[ZJxcGG|ZTDtbYNzd3S3YoXs[ZM> NIrzN2czOzd7OE[4NC=>
MCF-7 NG\hfYhHfW6ldHnvckBie3OjeR?= NFLNfXQ{OCEQvF2= MlP6SG1UVw>? MWTpcoNz\WG|ZYOgeIhmKGKrbnTpcochd2ZiSFTBR|Yhf2m2aDDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? NYLBfW4{OjN5OUi2PFA>
PC12 NEn1OpdHfW6ldHnvckBie3OjeR?= M3\XUp4{KM7:TR?= NIDNemxFVVOR NVvqPXVVfXBvcnXneYxifGW|IHHueIkud3irZHH0bZZmKGenbnWg[ZhxemW|c3nvckBz\WyjdHXkJJRwKHS{YX7zZ5JqeHSrb36g[oFkfG:{IGjCVFF{ M3zqS|I1QTB7Nki2
PC12 NVyyXHRVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4Hofp4{KM7:TR?= NWrNOG1WTE2VTx?= NYjKb3VWemW4ZYLz[UBJOk9{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NEjtPIszPDlyOU[4Oi=>
HEK293T NXXIe3c1TnWwY4Tpc44h[XO|YYm= NEHJNXh,OyEQvF2= NWnQWYNTTE2VTx?= MWf1dE1z\We3bHH0[YQhYEKSMYOgdJJwfGWrbjDs[ZZmdA>? NFz6T2wzPDlyOU[4Oi=>
HEK293T Mn;HSpVv[3Srb36gZZN{[Xl? NV7BcXIzhjNizszN NGTUTWJFVVOR NGTqOI9l\WyjeYOgXGJROXNicILveIVqdiCmZXfyZYRifGmxbjD2bYEh[WOndInsZZRqd25vbXXkbYF1\WRicILveIVie2:vYXyg[IVoemGmYYTpc44> NHnUeZUzPDlyOU[4Oi=>
Huh7 NYLKO21oTnWwY4Tpc44h[XO|YYm= MWL+OUDPxE1? MlrhSG1UVw>? Mknod5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:wIH;mJIhmeGG2aYTpd{BEKH[rcoXzJJJmeGyrY3;uJJdqfGhiRVO1NEA:KDBwMzFOwG0> NX3DPHRIOjVzMEizNlY>
SKMEL21 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXvTVplwhjVyMDDuUS=> M4jtUmROW09? NY[5SJpNcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NXvwRmExOjV7NUe4NVI>
SKMEL103 NUm1U4JIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NET0dW9,PTByIH7N MWXEUXNQ M4G2T4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M3LUfVI2QTV5OEGy
SKMEL28 MkPxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1HZXJ42ODBibl2= NVK3dYVDTE2VTx?= M1nWcIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NXvMcJc4OjV7NUe4NVI>
WM164 NVnNdZd[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWP+OVAxKG6P M2PvXWROW09? MnvhbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NUHFVJlyOjV7NUe4NVI>
WM1361a M4jYcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV3+OVAxKG6P M162VmROW09? NV;DT3U2cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MmnENlU6PTd6MUK=
WM1366 NFW0WIpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn7zglUxOCCwTR?= MnvZSG1UVw>? MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MkmwNlU6PTd6MUK=
WM793 MnPFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXr+OVAxKG6P M4\wZWROW09? M3PYO4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NUS1Wok2OjV7NUe4NVI>
WM35 NYq1W2dvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFO2OVV,PTByIH7N MWjEUXNQ MmXUbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M4OzN|I2QTV5OEGy
WM983a MmjUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkXlglUxOCCwTR?= NHHkUGpFVVOR NVvwbmpQcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MXmyOVk2PzhzMh?=
WM793 MoTiSpVv[3Srb36gZZN{[Xl? MnfyglYh|ryP MlriSG1UVw>? NXLjOo12cW6mdXPlJGcyKGG{cnXzeC=> MoHZNlU6PTd6MUK=
WM164 MlHmSpVv[3Srb36gZZN{[Xl? M{nK[543KM7:TR?= NETRNGpFVVOR MV7pcoR2[2ViR{GgZZJz\XO2 NVXDNXNbOjV7NUe4NVI>
WM983a M4j1b2Z2dmO2aX;uJIF{e2G7 NGLpeGh,PiEQvF2= NVnQTIdJTE2VTx?= Mn3GbY5lfWOnIFexJIFzemW|dB?= M2TvR|I2QTV5OEGy
WM164 MUHGeY5kfGmxbjDhd5NigQ>? NFzRWGN,OyEQvF2= NGHIb5JFVVOR Ml3hZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? MUSyOVk2PzhzMh?=
WM983a NWO0SmZLTnWwY4Tpc44h[XO|YYm= NHq1clB,OyEQvF2= MUnEUXNQ M2KwWoF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? MX6yOVk2PzhzMh?=
IPC298 NGHBZWhHfW6ldHnvckBie3OjeR?= MXf+N{DPxE1? MWHEUXNQ M1XIU4F2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? MWOyOVk2PzhzMh?=
SKMEL30 NEewe5JHfW6ldHnvckBie3OjeR?= M1TJOJ4{KM7:TR?= M{jETWROW09? NInRO|RifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| NI\PcYYzPTl3N{ixNi=>
TCa83 MlS2SpVv[3Srb36gZZN{[Xl? M3\yNolv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w MlzrNlYzPzl|MEO=
293T M4DHRmZ2dmO2aX;uJIF{e2G7 MV;+NkDPxGdxbXy= NV7Lbld5cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= MWGyOlI4QTNyMx?=
SACC-83 MmPiSpVv[3Srb36gZZN{[Xl? NHe0WYR,OiEQvHevcYw> M4TpXolv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NEjSXXUzPjJ5OUOwNy=>
293T NWTYNpNnTnWwY4Tpc44h[XO|YYm= NEWzWYZ,OiEQvHevcYw> M17Ub4lv\HWlZYOgVHRGViCjY3X0fYxifGmxbjDheEBMOTZ| MV6yOlI4QTNyMx?=
U-87 MG NFnPRmZHfW6ldHnvckBie3OjeR?= M3GxRZ4zKM7:Zz;tcC=> NUDZdIdMcW6qaXLpeJMhfGinIH3p[5JifGmxbjDhcoQhcW64YYPpc44> NH7yb24zPjJ5OUOwNy=>
U-87 MG NIjTbJRHfW6ldHnvckBie3OjeR?= MUn+NVAh|ryP MX3pcohq[mm2czDBT3QheGixc4Doc5J6dGG2aX;u NGj1VXIzPjJ5OUOwNy=>
U-87 MG MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF[4c45,OTBizszN Mm\0bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MkTINlYzPzl|MEO=

... 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 to the product individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
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