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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Cited by 21 Publications

Purity & Quality Control

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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 M1HtOWtqdmG|ZTDhd5NigQ>? NYCzNolnOi53IN88US=> MnnrSG1UVw>? MlGwbY5lfWOnczFOtU11fWK3bHnuJIh6eGW{YXPleJlt[XSrb36= M3;vTlIxPjF2OUO2
neuron cultures NFvFeXNHfW6ldHnvckBie3OjeR?= NWq1d4NNhjFyIN88US=> NWjvbZV{TE2VTx?= MkXzdJJwfGWldIOgZYdicW6|dDDncJV1[XSqaX;u[UBl\XCuZYTpc44ucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz Mlq5NlA3OTR7M{[=
134/04 NEX5RoFHfW6ldHnvckBie3OjeR?= NIPLXmk4NjViwsXN NInlWndqdXCjaYLzJI16d3S3YnWg[o9zdWG2aX;u M{jKZ|IzOTd2OEO5
C2C12 MYfGeY5kfGmxbjDhd5NigQ>? NGLWeVg4NjViwsXN MmjSbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= M4LlNlIzOTd2OEO5
HaCaT keratinocytes MUjGeY5kfGmxbjDhd5NigQ>? NEe5TocyOCEQvF2= NH;PemhjdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> MVyyNlM3PzZ6OR?=
JURL-MK1 MoLLSpVv[3Srb36gZZN{[Xl? NW[3eYFQOTBizszN M{PTcYVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NHvJTWMzOzB{MkW4Ny=>
CML-T1 NUn4O5BTTnWwY4Tpc44h[XO|YYm= MoHONVAh|ryP MVHlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MnPzNlMxOjJ3OEO=
K562 M1jidGZ2dmO2aX;uJIF{e2G7 NH30[mYyOCEQvF2= NVmxOWhX\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw MV:yN|AzOjV6Mx?=
HL-60 NX[2fZNbTnWwY4Tpc44h[XO|YYm= NUS4fmtnOTBizszN NGfMU2tmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? M2rhSFI{ODJ{NUiz
KMCH NYGwRpFiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mnz0glExKM7:TR?= MVfk[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> M4jjS|I{OzdyM{K3
THP-1 NG[3enRHfW6ldHnvckBie3OjeR?= MWr+NVAh|ryP M2j4eolvcGmkaYTzJHRPTi4QsTDhcoQhUUxvNjDz[YNz\XSrb36= NUG0[2Z5OjN3NEG2N|Q>
RAW 264.7 M3TR[GZ2dmO2aX;uJIF{e2G7 NVPqNYRXhjFyIN88US=> NXq2VG9q[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u NG\MUY8zOzV2MU[zOC=>
HT3 MnjqSpVv[3Srb36gZZN{[Xl? MYH+OUDPxE1? MnnpSG1UVw>? NYnlbXR7cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? MXSyN|Y6QDR4OB?=
SiHa Mnz6SpVv[3Srb36gZZN{[Xl? MnfvglUh|ryP M1XpO2ROW09? MorEbY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> MVOyN|Y6QDR4OB?=
CaSki NUTuflh4TnWwY4Tpc44h[XO|YYm= M37Jc542KM7:TR?= M2\4VGROW09? MX3pcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> NVj3R|RHOjN4OUi0Olg>
SiHa MWnGeY5kfGmxbjDhd5NigQ>? M2HacJ42KM7:TR?= M4TuTGROW09? M3jRUolvcGmkaYTzJHRp[XC|aXfhdodqdi1ib4KgSWdHNWmwZIXj[YQhW0:FRTDhZ5RqfmG2aX;u NX71[nljOjN4OUi0Olg>
CaSki NEj5OXVHfW6ldHnvckBie3OjeR?= MnK3glUh|ryP MVrEUXNQ NUn5bGxwcW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> MVqyN|Y6QDR4OB?=
MCF-7 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Ml\kN|Ah|ryP MlvzSG1UVw>? NXjj[VJmUUN3ME2xOUDPxE1? MYKyN|c6QDZ6MB?=
MCF-7 NWq5VoRkTnWwY4Tpc44h[XO|YYm= NVGyeVRYOzBizszN NVXB[lBITE2VTx?= NHLCc3JqdmO{ZXHz[ZMhfGinIH3pZ5JwfHWkdXzlJIFk\XS7bHH0bY9vKGyndnXsMi=> Ml[3NlM4QTh4OEC=
MCF-7 MnHiSpVv[3Srb36gZZN{[Xl? NHjHT|k{OCEQvF2= NETjT29FVVOR MVjzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KGOxbHStbY5lfWOnZDDk[ZBwdHmvZYLpfoF1cW:w MnHRNlM4QTh4OEC=
MCF-7 NFfU[IFHfW6ldHnvckBie3OjeR?= NYi3WYhKOTVizszN MV3EUXNQ MnXZd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCCwb3Pv[IF7d2ynLXnu[JVk\WRiZHnzZZN{\W2kbIm= MnHhNlM4QTh4OEC=
MCF-7 MXnGeY5kfGmxbjDhd5NigQ>? MW[zNEDPxE1? NX\GdWJmTE2VTx?= MVvhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> MmPCNlM4QTh4OEC=
MCF-7 M4i2VWZ2dmO2aX;uJIF{e2G7 NX;Sc4tUOzBizszN NUPuc4JJTE2VTx?= MYHpcoNz\WG|ZYOgeIhmKGKrbnTpcochd2ZiSFTBR|Yhf2m2aDDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? NGfUdnkzOzd7OE[4NC=>
PC12 Mmq3SpVv[3Srb36gZZN{[Xl? MYL+N{DPxE1? NX7JdXJKTE2VTx?= NWXlfHp4fXBvcnXneYxifGW|IHHueIkud3irZHH0bZZmKGenbnWg[ZhxemW|c3nvckBz\WyjdHXkJJRwKHS{YX7zZ5JqeHSrb36g[oFkfG:{IGjCVFF{ M1LMNVI1QTB7Nki2
PC12 MkLpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmHuglMh|ryP MWTEUXNQ M3PjUJJmfmW{c3WgTFJQOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v MUCyOFkxQTZ6Nh?=
HEK293T NFL5RoVHfW6ldHnvckBie3OjeR?= NYLzRW9uhjNizszN NX7HeJZsTE2VTx?= NEmydG12eC2{ZXf1cIF1\WRiWFLQNZMheHKxdHXpckBt\X[nbB?= NFzsNZczPDlyOU[4Oi=>
HEK293T M37STmZ2dmO2aX;uJIF{e2G7 MWD+N{DPxE1? NH;rTmpFVVOR M2DBXYRmdGG7czDYRnAyeyCycn;0[YlvKGSnZ4Lh[IF1cW:wII\pZUBi[2W2eXzheIlwdi2vZXTpZZRm\CCycn;0[YF{d22jbDDk[Ydz[WSjdHnvci=> M3f5SVI1QTB7Nki2
Huh7 MljzSpVv[3Srb36gZZN{[Xl? MmqwglUh|ryP MV3EUXNQ M2rzd5N2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbjDv[kBp\XCjdHn0bZMhSyC4aYL1d{Bz\XCuaXPvckB4cXSqIFXDOVAhRSByLkOg{txO M4T6VlI2OTB6M{K2
SKMEL21 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmLBglUxOCCwTR?= NYTtTI1NTE2VTx?= M4XjZYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NX;oNWk4OjV7NUe4NVI>
SKMEL103 NHHyd3pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVT+OVAxKG6P Mle2SG1UVw>? NF:3U3dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NWnsPGdQOjV7NUe4NVI>
SKMEL28 MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1Htfp42ODBibl2= MV7EUXNQ NXfBelEzcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NEDscVMzPTl3N{ixNi=>
WM164 MlrlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFrG[Gt,PTByIH7N MkTiSG1UVw>? MkLnbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MmXqNlU6PTd6MUK=
WM1361a M2i5Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEL4UWd,PTByIH7N MoXZSG1UVw>? NUHzN2hpcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHfsWowzPTl3N{ixNi=>
WM1366 MmDiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVz+OVAxKG6P NVzOSZNsTE2VTx?= NVvPXYZCcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NXzhc2lzOjV7NUe4NVI>
WM793 MnzFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml\hglUxOCCwTR?= M1fCcmROW09? MkeybY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M{noXlI2QTV5OEGy
WM35 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXP+OVAxKG6P MmTQSG1UVw>? Ml;jbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MkW1NlU6PTd6MUK=
WM983a NF64bXFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHG1d|B,PTByIH7N NV7hOVltTE2VTx?= MYnpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= Ml7ZNlU6PTd6MUK=
WM793 M162bWZ2dmO2aX;uJIF{e2G7 MXL+OkDPxE1? NXTCZXBMTE2VTx?= Mn;lbY5lfWOnIFexJIFzemW|dB?= M3PRclI2QTV5OEGy
WM164 MlvKSpVv[3Srb36gZZN{[Xl? MmrxglYh|ryP MYfEUXNQ M4Dy[olv\HWlZTDHNUBienKnc4S= MmnQNlU6PTd6MUK=
WM983a NWHmRlk4TnWwY4Tpc44h[XO|YYm= MUX+OkDPxE1? NHXzeXVFVVOR NY[wSmxycW6mdXPlJGcyKGG{cnXzeC=> NGnBZoEzPTl3N{ixNi=>
WM164 M3vaPWZ2dmO2aX;uJIF{e2G7 MXr+N{DPxE1? M3TPbmROW09? M1PGPYF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? MYCyOVk2PzhzMh?=
WM983a M1jwfGZ2dmO2aX;uJIF{e2G7 M{jHTZ4{KM7:TR?= NUTUXZl5TE2VTx?= MnvFZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? M16yVlI2QTV5OEGy
IPC298 MUTGeY5kfGmxbjDhd5NigQ>? NV;1NIhqhjNizszN M1[3WmROW09? NX61OI1G[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NWXaOol4OjV7NUe4NVI>
SKMEL30 Mlf4SpVv[3Srb36gZZN{[Xl? MX\+N{DPxE1? NFrqR3ZFVVOR MkjNZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NVvWe|hQOjV7NUe4NVI>
TCa83 MYjGeY5kfGmxbjDhd5NigQ>? M1nac4lv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w MYiyOlI4QTNyMx?=
293T NX\oellTTnWwY4Tpc44h[XO|YYm= NV3FUIlYhjJizsznM41t NYHnenFMcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= M1zZSFI3Ojd7M{Cz
SACC-83 MVvGeY5kfGmxbjDhd5NigQ>? NILvblR,OiEQvHevcYw> NGS2[VlqdmS3Y3XzJHBVTU5iZYjwdoV{e2mxbjDhcoQhdWWvYoLhcoUhfHKjboPsc4NifGmxbh?= NIfqOmUzPjJ5OUOwNy=>
293T NHGzSFVHfW6ldHnvckBie3OjeR?= MVf+NkDPxGdxbXy= M2W3PIlv\HWlZYOgVHRGViCjY3X0fYxifGmxbjDheEBMOTZ| NF\TRYkzPjJ5OUOwNy=>
U-87 MG NYL0dZpKTnWwY4Tpc44h[XO|YYm= MXv+NkDPxGdxbXy= NEHkN25qdmirYnn0d{B1cGVibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> M13QTlI3Ojd7M{Cz
U-87 MG M3XGUGZ2dmO2aX;uJIF{e2G7 NG\oeYx,OTBizszN MnLIbY5pcWKrdIOgRWtVKHCqb4PwbI9zgWyjdHnvci=> NVzPZmQyOjZ{N{mzNFM>
U-87 MG NWPXWJVmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnTlglExKM7:TR?= M2rnXIlvcGmkaYTzJINmdGxiZ4Lve5Rp NUT3NXdmOjZ{N{mzNFM>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
EGFR / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29665050     


In KYSE140 (C) and KYSE180 (D), Tubastatin treatment EGFR, AKT, phospho-AKT and phospho-ERK levels were decreased in tubastatin-treated cells compared with control group.

29665050
Immunofluorescence
α-tubulin / Acetylated tubulin ; 

PubMed: 23798680     


Effects of tubastatin A on microtubules and microtubule acetylation level are shown. MCF-7 cells were treated with different concentrations of tubastatin A for 24 h and processed for immunostaining with antibodies against α-tubulin (green) and acetylated tubulin (red). Scale bars, 10 μm.

HDAC6; 

PubMed: 23798680     


MCF-7 cells are treated with vehicle, 30 μm tubastatin A (TBA), or 240 nm TSA for 24 h and fixed and processed to visualize microtubules (red) and HDAC6 (green). Scale bar, 20 μm.

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

Kinase Assay:[1]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID