Tubastatin A HCl

For research use only. Not for use in humans.

Catalog No.S2627

21 publications

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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Selleck's Tubastatin A HCl has been cited by 21 publications

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 MnyxT4lv[XOnIHHzd4F6 NULtR5VLOi53IN88US=> Mk\rSG1UVw>? NFnESXdqdmS3Y3XzJO6yNXS3YoXsbY4hcHmyZYLhZ4V1gWyjdHnvci=> NH:5NlYzODZzNEmzOi=>
neuron cultures NFLrbFFHfW6ldHnvckBie3OjeR?= MYP+NVAh|ryP MXPEUXNQ M1;D[JBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGG2aHnvcoUh\GWybHX0bY9vNWmwZIXj[YQhd3irZHH0bZZmKHO2cnXzdy=> MXqyNFYyPDl|Nh?=
134/04 NXH4TWtSTnWwY4Tpc44h[XO|YYm= NVPjTW9iPy53INM1US=> NGPYXo1qdXCjaYLzJI16d3S3YnWg[o9zdWG2aX;u NYjJdFFUOjJzN{S4N|k>
C2C12 MXXGeY5kfGmxbjDhd5NigQ>? MlmyO{42KML3TR?= NHrHW5dqdXCjaYLzJI16d3S3YnWg[o9zdWG2aX;u M4H2W|IzOTd2OEO5
HaCaT keratinocytes NHXFepVHfW6ldHnvckBie3OjeR?= NV3seVhtOTBizszN NIf4cWZjdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> NF\RfIEzOjN4N{[4PS=>
JURL-MK1 MUfGeY5kfGmxbjDhd5NigQ>? MY[xNEDPxE1? MX\lcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> M4CweFI{ODJ{NUiz
CML-T1 NFLkXmZHfW6ldHnvckBie3OjeR?= NUHkXXZ5OTBizszN NYqxblBj\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw Ml;GNlMxOjJ3OEO=
K562 M1zrXWZ2dmO2aX;uJIF{e2G7 MYmxNEDPxE1? NX[yboJD\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw M3j1RVI{ODJ{NUiz
HL-60 MmrTSpVv[3Srb36gZZN{[Xl? NX3QZW0xOTBizszN M3TYN4VvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? M{\IRVI{ODJ{NUiz
KMCH NXX6cHVnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUTFeJRlhjFyIN88US=> MV3k[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> NY\hRW02OjN|N{CzNlc>
THP-1 NHH5bGlHfW6ldHnvckBie3OjeR?= MoH6glExKM7:TR?= MmmzbY5pcWKrdIOgWG5HNc7zIHHu[EBKVC14IIPlZ5JmfGmxbh?= MV6yN|U1OTZ|NB?=
RAW 264.7 NXKxTVk{TnWwY4Tpc44h[XO|YYm= NGjSXmJ,OTBizszN NUnRfmlz[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u M3L4WVI{PTRzNkO0
HT3 NGezbVBHfW6ldHnvckBie3OjeR?= NYG4NVZ7hjVizszN MlT0SG1UVw>? M4raVolv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v M2O5eVI{Pjl6NE[4
SiHa M4LZTWZ2dmO2aX;uJIF{e2G7 NInF[Jp,PSEQvF2= MV\EUXNQ M2\uVYlv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v NULGN3ZYOjN4OUi0Olg>
CaSki NUDpcpBvTnWwY4Tpc44h[XO|YYm= NYnEe2VHhjVizszN MVzEUXNQ MVvpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> M{f3dVI{Pjl6NE[4
SiHa MkK0SpVv[3Srb36gZZN{[Xl? M3Ptfp42KM7:TR?= NHi3XGJFVVOR M3S0Z4lvcGmkaYTzJHRp[XC|aXfhdodqdi1ib4KgSWdHNWmwZIXj[YQhW0:FRTDhZ5RqfmG2aX;u MVGyN|Y6QDR4OB?=
CaSki NHjtd5VHfW6ldHnvckBie3OjeR?= MlXlglUh|ryP MXzEUXNQ NIjOdFVqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> M3fyPVI{Pjl6NE[4
MCF-7 NVHaTFNtT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1zQWlMxKM7:TR?= MkL2SG1UVw>? MUPJR|UxRTF3IN88US=> MXWyN|c6QDZ6MB?=
MCF-7 NHrxdFZHfW6ldHnvckBie3OjeR?= M2PuWVMxKM7:TR?= MXXEUXNQ MojGbY5kemWjc3XzJJRp\SCvaXPyc5R2[nWuZTDhZ4V1gWyjdHnvckBt\X[nbD6= NWHIXZpVOjN5OUi2PFA>
MCF-7 M{[yRmZ2dmO2aX;uJIF{e2G7 NELqSYg{OCEQvF2= NGHSS29FVVOR NIXsemh{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IHPvcIQucW6mdXPl[EBl\XCxbInt[ZJqgmG2aX;u NILhT4IzOzd7OE[4NC=>
MCF-7 M4PEV2Z2dmO2aX;uJIF{e2G7 MlPONVUh|ryP MkCxSG1UVw>? NHjWTol{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IH7vZ49l[XqxbHWtbY5lfWOnZDDkbZNie3OnbXLsfS=> NED1UGUzOzd7OE[4NC=>
MCF-7 NGPPSlJHfW6ldHnvckBie3OjeR?= MojFN|Ah|ryP MnS0SG1UVw>? NXTaZ2ZR[Wy2ZYLld{B1cGViYYPz[Y1jdHliZInuZY1q[3Nib3[gbY51\XKyaHHz[UBucWO{b4T1ZpVt\XN? NVzFPWcyOjN5OUi2PFA>
MCF-7 NIXib4lHfW6ldHnvckBie3OjeR?= MYCzNEDPxE1? MUTEUXNQ MVLpcoNz\WG|ZYOgeIhmKGKrbnTpcochd2ZiSFTBR|Yhf2m2aDDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? NUXMWWF[OjN5OUi2PFA>
PC12 NIm0VHNHfW6ldHnvckBie3OjeR?= MmHoglMh|ryP NYrDemY6TE2VTx?= NEjVUXZ2eC2{ZXf1cIF1\XNiYX70bU1wgGmmYYTpeoUh\2WwZTDlfJBz\XO|aX;uJJJmdGG2ZXSgeI8hfHKjboPjdolxfGmxbjDmZYN1d3JiWFLQNZM> NHf1flgzPDlyOU[4Oi=>
PC12 NUf1SIJrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2e3UJ4{KM7:TR?= M4rFcmROW09? MYDy[ZZmenOnIFiyU|IucW6mdXPl[EBoem:5dHigbY5pcWKrdHnvci=> NHOyWpQzPDlyOU[4Oi=>
HEK293T M2TNNWZ2dmO2aX;uJIF{e2G7 NYXrWGJ5hjNizszN NXzlZ4tkTE2VTx?= NW\xXmFlfXBvcnXneYxifGWmIGjCVFF{KHC{b4TlbY4hdGW4ZXy= Ml3YNlQ6ODl4OE[=
HEK293T Mn3tSpVv[3Srb36gZZN{[Xl? NUP5Z4N[hjNizszN NGrScVRFVVOR MljX[IVt[Xm|IGjCVFF{KHC{b4TlbY4h\GWpcnHkZZRqd25idnnhJIFk\XS7bHH0bY9vNW2nZHnheIVlKHC{b4TlZZNwdWGuIHTl[5Ji\GG2aX;u MWGyOFkxQTZ6Nh?=
Huh7 M1LmV2Z2dmO2aX;uJIF{e2G7 MoX1glUh|ryP Mle5SG1UVw>? M{XEeJN2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbjDv[kBp\XCjdHn0bZMhSyC4aYL1d{Bz\XCuaXPvckB4cXSqIFXDOVAhRSByLkOg{txO MkHONlUyODh|Mk[=
SKMEL21 NVzmWmZlT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEDNclF,PTByIH7N MVzEUXNQ MYTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MXeyOVk2PzhzMh?=
SKMEL103 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1zhT542ODBibl2= NF;MfHZFVVOR NEDsOZpqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MWeyOVk2PzhzMh?=
SKMEL28 MWXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUX+OVAxKG6P NXezS5d4TE2VTx?= M4nHb4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MmDNNlU6PTd6MUK=
WM164 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXX+OVAxKG6P MXXEUXNQ MmGzbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MlPxNlU6PTd6MUK=
WM1361a M1noNWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1;hZZ42ODBibl2= MkTKSG1UVw>? MVzpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NUT4NXFTOjV7NUe4NVI>
WM1366 NXG0eVNsT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlPPglUxOCCwTR?= MWnEUXNQ MojvbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NUTFc5Z7OjV7NUe4NVI>
WM793 M3PpXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIDIb3J,PTByIH7N NIj1Z5FFVVOR Mni4bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M4GwOlI2QTV5OEGy
WM35 NFXXSnFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYX+OVAxKG6P NHfVZYxFVVOR M1W0OolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M3fGfVI2QTV5OEGy
WM983a NGjKV2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYP+OVAxKG6P MknaSG1UVw>? Ml\nbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NHPlO4IzPTl3N{ixNi=>
WM793 NIC1TGJHfW6ldHnvckBie3OjeR?= NXrQU201hjZizszN MXHEUXNQ M3jJO4lv\HWlZTDHNUBienKnc4S= NVO0R2Y2OjV7NUe4NVI>
WM164 MoP6SpVv[3Srb36gZZN{[Xl? NWjHXnk1hjZizszN NWH4eW5jTE2VTx?= NXr2THc6cW6mdXPlJGcyKGG{cnXzeC=> MkDyNlU6PTd6MUK=
WM983a MoGxSpVv[3Srb36gZZN{[Xl? NVrRcJZWhjZizszN MXvEUXNQ M3\xTolv\HWlZTDHNUBienKnc4S= MXyyOVk2PzhzMh?=
WM164 NIDNOoxHfW6ldHnvckBie3OjeR?= NUjreGpXhjNizszN Mn30SG1UVw>? Mk\qZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NFn5OYMzPTl3N{ixNi=>
WM983a MmLDSpVv[3Srb36gZZN{[Xl? M{T1Up4{KM7:TR?= NGe3O|hFVVOR NELKeYJifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| MYWyOVk2PzhzMh?=
IPC298 NWewTHBuTnWwY4Tpc44h[XO|YYm= MUP+N{DPxE1? MoPkSG1UVw>? NU\kXZQ{[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NF;uSoQzPTl3N{ixNi=>
SKMEL30 MmH2SpVv[3Srb36gZZN{[Xl? M3qzd54{KM7:TR?= M{m0PWROW09? NVvsTpIy[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NYTXflNVOjV7NUe4NVI>
TCa83 Ml7NSpVv[3Srb36gZZN{[Xl? M2PpO4lv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NYDtb4RsOjZ{N{mzNFM>
293T MnjJSpVv[3Srb36gZZN{[Xl? NUfYflZshjJizsznM41t NXrPdVdCcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NI\MbJEzPjJ5OUOwNy=>
SACC-83 MknYSpVv[3Srb36gZZN{[Xl? MVP+NkDPxGdxbXy= M2rtOYlv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NH7F[nkzPjJ5OUOwNy=>
293T MlK0SpVv[3Srb36gZZN{[Xl? NWrSNlB1hjJizsznM41t M3r0[Ilv\HWlZYOgVHRGViCjY3X0fYxifGmxbjDheEBMOTZ| M{\pO|I3Ojd7M{Cz
U-87 MG MXHGeY5kfGmxbjDhd5NigQ>? NHnDUVF,OiEQvHevcYw> NXu2PGJFcW6qaXLpeJMhfGinIH3p[5JifGmxbjDhcoQhcW64YYPpc44> NF3s[lYzPjJ5OUOwNy=>
U-87 MG MWLGeY5kfGmxbjDhd5NigQ>? Mn\5glExKM7:TR?= MlvjbY5pcWKrdIOgRWtVKHCqb4PwbI9zgWyjdHnvci=> NYPsW25tOjZ{N{mzNFM>
U-87 MG M2XXOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWXjS25EhjFyIN88US=> MWXpcohq[mm2czDj[YxtKGe{b4f0bC=> MYWyOlI4QTNyMx?=

... 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]
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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]
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  • 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
Smiles Cl.CN1CCC2=C(C1)C3=C(C=CC=C3)[N]2CC4=CC=C(C=C4)C(=O)NO

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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