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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In DMSO USD 160 In stock
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2 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
15 nM 854 nM 16.4 μM >30 μM >30 μM
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 M4TERmtqdmG|ZTDhd5NigQ>? MUWyMlUh|ryP NInjbVRFVVOR M4KzVolv\HWlZYOg{tEufHWkdXzpckBpgXCncnHj[ZR6dGG2aX;u MVyyNFYyPDl|Nh?=
neuron cultures MXjGeY5kfGmxbjDhd5NigQ>? NUmxVXBShjFyIN88US=> NUnxdYx5TE2VTx?= M1ziO5Bzd3SnY4TzJIFo[Wmwc4Sg[4x2fGG2aHnvcoUh\GWybHX0bY9vNWmwZIXj[YQhd3irZHH0bZZmKHO2cnXzdy=> NGT5eYgzODZzNEmzOi=>
134/04 NFXqSnpHfW6ldHnvckBie3OjeR?= Mn:wO{42KML3TR?= MmnsbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= MoLuNlIyPzR6M{m=
C2C12 MnzQSpVv[3Srb36gZZN{[Xl? Ml7TO{42KML3TR?= NYDDc2Z3cW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> M33WU|IzOTd2OEO5
HaCaT keratinocytes NYHDbXBuTnWwY4Tpc44h[XO|YYm= Ml62NVAh|ryP MYLicI9kc3NiYYLz[Y5qfGViZoLvcUBqdmS3Y3nu[{BPemZ{IIDyc5RmcW5idILhcpNt[XSrb36= M3W2TVIzOzZ5Nki5
JURL-MK1 MVfGeY5kfGmxbjDhd5NigQ>? MXixNEDPxE1? M33ab4VvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NFnZfowzOzB{MkW4Ny=>
CML-T1 NFThZnZHfW6ldHnvckBie3OjeR?= M3TiclExKM7:TR?= NGT6VIpmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? NWfsW2psOjNyMkK1PFM>
K562 MnzuSpVv[3Srb36gZZN{[Xl? NXvWeW5MOTBizszN NGe4U5NmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MVyyN|AzOjV6Mx?=
HL-60 M2\vfGZ2dmO2aX;uJIF{e2G7 M2WxXlExKM7:TR?= NILqRnFmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MUmyN|AzOjV6Mx?=
KMCH NX7OSFVHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2Oxbp4yOCEQvF2= M2DMdYRm[3KnYYPld{Bxem:uaX\ldoF1cW:wIHHu[EBidmOqb4Lh[4UucW6mZYDlcoRmdnRiZ4Lve5Rp Mm\xNlM{PzB|Mke=
THP-1 MoDnSpVv[3Srb36gZZN{[Xl? MVX+NVAh|ryP M4m0XIlvcGmkaYTzJHRPTi4QsTDhcoQhUUxvNjDz[YNz\XSrb36= MVKyN|U1OTZ|NB?=
RAW 264.7 NV:zOHU1TnWwY4Tpc44h[XO|YYm= M{nHVp4yOCEQvF2= MWHheJRmdnWjdHXzJG5QKHC{b3T1Z5Rqd25? MoewNlM2PDF4M{S=
HT3 M3zITWZ2dmO2aX;uJIF{e2G7 NGC3ZVl,PSEQvF2= M1rCTGROW09? MULpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> NWe3SWxGOjN4OUi0Olg>
SiHa NX\H[IRtTnWwY4Tpc44h[XO|YYm= MVX+OUDPxE1? MoHtSG1UVw>? M{O4c4lv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v MUWyN|Y6QDR4OB?=
CaSki NXnEOXJsTnWwY4Tpc44h[XO|YYm= M4[xUZ42KM7:TR?= M3\zRmROW09? NHfYdWdqdmS3Y3XzJJRp\SCmaX\m[ZJmdnSrYXyg{tEufHWkdXzpckBi[2W2eXzheIlwdg>? NWLKN5dKOjN4OUi0Olg>
SiHa MWHGeY5kfGmxbjDhd5NigQ>? NXP3Zm01hjVizszN MkLMSG1UVw>? NHfQT4JqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> NGSxbW0zOzZ7OES2PC=>
CaSki MXnGeY5kfGmxbjDhd5NigQ>? M2nCPJ42KM7:TR?= Mn\4SG1UVw>? M{DRTolvcGmkaYTzJHRp[XC|aXfhdodqdi1ib4KgSWdHNWmwZIXj[YQhW0:FRTDhZ5RqfmG2aX;u NWHXfGtwOjN4OUi0Olg>
MCF-7 Mn3GS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlfWN|Ah|ryP NYLjdI1CTE2VTx?= NV6xWnVUUUN3ME2xOUDPxE1? MWmyN|c6QDZ6MB?=
MCF-7 M3jnVmZ2dmO2aX;uJIF{e2G7 NWG5VHZ[OzBizszN NXLLTnRtTE2VTx?= NVy5OoRYcW6lcnXhd4V{KHSqZTDtbYNzd3S3YoXs[UBi[2W2eXzheIlwdiCuZY\lcE4> MYKyN|c6QDZ6MB?=
MCF-7 MV\GeY5kfGmxbjDhd5NigQ>? Mn\lN|Ah|ryP NUPOfWY{TE2VTx?= NWfwRY1Qe3SjYnnsbZpmeyCvaXPyc5R2[nWuZYOgZYdicW6|dDDjc4xlNWmwZIXj[YQh\GWyb3z5cYVzcXqjdHnvci=> NFrtVJUzOzd7OE[4NC=>
MCF-7 NG\se25HfW6ldHnvckBie3OjeR?= NFu4ToUyPSEQvF2= NVy0UIZvTE2VTx?= MUTzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KG6xY3;kZZpwdGVvaX7keYNm\CCmaYPhd5NmdWKueR?= MlX6NlM4QTh4OEC=
MCF-7 NUTmNFd[TnWwY4Tpc44h[XO|YYm= MUWzNEDPxE1? NVOzUm5DTE2VTx?= Mo\KZYx1\XKnczD0bIUh[XO|ZX3icJkh\HmwYX3pZ5Mhd2ZiaX70[ZJxcGG|ZTDtbYNzd3S3YoXs[ZM> NFjSdpAzOzd7OE[4NC=>
MCF-7 NYfLeIhkTnWwY4Tpc44h[XO|YYm= Mmr2N|Ah|ryP NGrOc|lFVVOR NGOyN4RqdmO{ZXHz[ZMhfGinIHLpcoRqdmdib3[gTGRCSzZid3n0bEBqdnSncoDoZZNmKG2rY4LveJVjfWyncx?= MojMNlM4QTh4OEC=
PC12 M1zG[WZ2dmO2aX;uJIF{e2G7 NUPMbGxxhjNizszN M3;mPWROW09? MYH1dE1z\We3bHH0[ZMh[W62aT3vfIll[XSrdnWg[4Vv\SCneIDy[ZN{cW:wIILlcIF1\WRidH:geJJidnOlcnnweIlwdiCoYXP0c5IhYEKSMYO= MV[yOFkxQTZ6Nh?=
PC12 NU\weo01T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NE[wTmp,OyEQvF2= MoC1SG1UVw>? NX7Ke5RxemW4ZYLz[UBJOk9{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? Ml;3NlQ6ODl4OE[=
HEK293T NEXvVZpHfW6ldHnvckBie3OjeR?= NIn0eGV,OyEQvF2= MVvEUXNQ Ml;neZAuemWpdXzheIVlKFiEUEHzJJBzd3SnaX6gcIV3\Wx? M{jubVI1QTB7Nki2
HEK293T MX;GeY5kfGmxbjDhd5NigQ>? NVG4coV6hjNizszN M1LRbmROW09? NVLRbJhZ\GWuYYnzJHhDWDG|IIDyc5RmcW5iZHXndoFl[XSrb36geoliKGGlZYT5cIF1cW:wLX3l[IlifGWmIIDyc5Rm[XOxbXHsJIRm\3KjZHH0bY9v NWPpOm1qOjR7MEm2PFY>
Huh7 NILkXIhHfW6ldHnvckBie3OjeR?= Mlj0glUh|ryP MX;EUXNQ NGrnOIF{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36gc4YhcGWyYYTpeIl{KENidnnyeZMhemWybHnjc44hf2m2aDDFR|UxKD1iMD6zJO69VQ>? MoC0NlUyODh|Mk[=
SKMEL21 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX\+OVAxKG6P MWHEUXNQ MnWxbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MoixNlU6PTd6MUK=
SKMEL103 M2nobGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M362XZ42ODBibl2= NEDKdmdFVVOR MorqbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M{\Fe|I2QTV5OEGy
SKMEL28 NVvNU21WT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NULlR|U1hjVyMDDuUS=> MUPEUXNQ M{\udYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NYPzeJpUOjV7NUe4NVI>
WM164 MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYnWXooyhjVyMDDuUS=> NFTlcJpFVVOR NHLBe3RqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MVOyOVk2PzhzMh?=
WM1361a M{HE[mdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWXNXY9MhjVyMDDuUS=> NFTUUFlFVVOR MljWbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NGK2VFUzPTl3N{ixNi=>
WM1366 NV;T[lZwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NH;6TYl,PTByIH7N NX;ERZg6TE2VTx?= MlewbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NH21[pYzPTl3N{ixNi=>
WM793 NF;IfnhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mk\hglUxOCCwTR?= MXzEUXNQ MonDbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MkXKNlU6PTd6MUK=
WM35 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1jFZ542ODBibl2= NWqxcmplTE2VTx?= Mk\hbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MnnsNlU6PTd6MUK=
WM983a NXzVc4ZHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVr+OVAxKG6P MoP1SG1UVw>? Mk[4bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NYHNZXFXOjV7NUe4NVI>
WM793 NXT2c|hzTnWwY4Tpc44h[XO|YYm= MoTGglYh|ryP NVXMXY9lTE2VTx?= NVTVOJU4cW6mdXPlJGcyKGG{cnXzeC=> M4rkNFI2QTV5OEGy
WM164 MX;GeY5kfGmxbjDhd5NigQ>? NV\qRZN5hjZizszN NU\vVHh1TE2VTx?= MXrpcoR2[2ViR{GgZZJz\XO2 NHLrcnkzPTl3N{ixNi=>
WM983a M3fBZWZ2dmO2aX;uJIF{e2G7 MmrJglYh|ryP NH\Vc21FVVOR MYXpcoR2[2ViR{GgZZJz\XO2 NFP6R48zPTl3N{ixNi=>
WM164 MlOwSpVv[3Srb36gZZN{[Xl? MmjrglMh|ryP NH34TopFVVOR MmrvZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? MkPKNlU6PTd6MUK=
WM983a M4DXT2Z2dmO2aX;uJIF{e2G7 MYX+N{DPxE1? Mo\4SG1UVw>? Ml\kZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NIjoSVYzPTl3N{ixNi=>
IPC298 MWnGeY5kfGmxbjDhd5NigQ>? Mo\FglMh|ryP MXfEUXNQ M{X5eoF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? MVOyOVk2PzhzMh?=
SKMEL30 Ml7aSpVv[3Srb36gZZN{[Xl? MoHSglMh|ryP NI\1SY5FVVOR M3PrSIF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? M1nTe|I2QTV5OEGy
TCa83 NX3ndpExTnWwY4Tpc44h[XO|YYm= M2H3PIlv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NF;QNW4zPjJ5OUOwNy=>
293T MVjGeY5kfGmxbjDhd5NigQ>? M1u2XJ4zKM7:Zz;tcC=> M2fYSIlv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NV3WbVBqOjZ{N{mzNFM>
SACC-83 MlywSpVv[3Srb36gZZN{[Xl? Ml7tglIh|rypL33s NV;hbZE5cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= M3L2SFI3Ojd7M{Cz
293T NEDsXFlHfW6ldHnvckBie3OjeR?= NW\yU5k1hjJizsznM41t NIq2cWFqdmS3Y3XzJHBVTU5iYXPleJlt[XSrb36gZZQhUzF4Mx?= MUWyOlI4QTNyMx?=
U-87 MG M3zWRmZ2dmO2aX;uJIF{e2G7 NY\VZXAxhjJizsznM41t NFv3dWJqdmirYnn0d{B1cGVibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> MVGyOlI4QTNyMx?=
U-87 MG M2X2WGZ2dmO2aX;uJIF{e2G7 NYrhN4xohjFyIN88US=> NVP1NpJWcW6qaXLpeJMhSUuWIIDoc5NxcG:{eXzheIlwdg>? M1P2T|I3Ojd7M{Cz
U-87 MG NYnoUpdOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4ftcp4yOCEQvF2= NXfzblVkcW6qaXLpeJMh[2WubDDndo94fGh? NFLuc2EzPjJ5OUOwNy=>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID