Mocetinostat (MGCD0103)

Catalog No.S1122 Synonyms: MG0103

Mocetinostat (MGCD0103) Chemical Structure

Molecular Weight(MW): 396.44

Mocetinostat (MGCD0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Phase 2.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 270 In stock
USD 470 In stock
USD 770 In stock

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6 Customer Reviews

  •  

    Comparison of MCAS ovarian cancer cells harboring control and CtBP2 knockdown shRNAs for sensitivity to chemotherapeutic agents. For each cell line, the MTT reading of the untreated cells was assigned as 100%. HDAC inhibitors: (a) Trichostatin A; (b) Vorinostat; (c) Belinostat; (d) MGCD0103; (e) valproic acid; and (f ) carboplatin, a non-HDAC inhibitor.

    Oncogene 2012 32, 3896-903. Mocetinostat (MGCD0103) purchased from Selleck.

    Class-specific histone deacetylase inhibition ameliorates cholesterol accumulation. Mutant fibroblasts (NPC-26) were incubated for 18 h in the presence of the HDAC class-specific inhibitors MC1568 and MGCD0103 (5 μM) and assessed for cholesterol accumulation by filipin fluorescence. Quantification of filipin fluorescence is expressed as arbitrary units. *, p<0.05, treated versus untreated cells by two-tailed Student,s t test.

    J Biol Chem 2011 286, 23842–23851. Mocetinostat (MGCD0103) purchased from Selleck.

  •  

    HDACI sensitivities in pancreatic cancer cell lines and the HPDE cells. Panels A–C: PANC-1 cells were harvested and lysed after incubation with a range of concentrations of MGCD0103 (0–1.0 uM), MC1568 (0–10 uM), or Tubastatin A (0–4 uM) for 96 h. Soluble proteins were analyzed on Western blots probed by anti-acetylated (ac)-H4, -H4, -ac-tubulin, or –b-actin antibody. Panel D: AsPC-1, BxPC-3, PANC-1, or the HPDE cells were cultured at 37’C for 96 h in complete medium in 96-well plates, with a range of concentrations of MGCD0103, MC1568, or Tubastatin A, and cell viabilities were determined using the MTT reagent.

    PLoS One 2012 7, e52095. Mocetinostat (MGCD0103) purchased from Selleck.

    HDACIs That Simultaneously Inhibit HDACs 1 and 6 Showed Greater Antileukemic Activities than HDACIs that Don,t at Cmax Concentrations. THP-1 cells were treated with LBH-589, PXD101, SAHA, VPA, MS-275 and MGCD0103 at Cmax concentrations for 3 h and 24 h, respectively. The cells post 3 h treatments were washed three times with complete medium and divided into two halves. One half of the cells was resuspended in complete media and cultured for up to 24 h to determine the effects of the 3 h treatments on cell proliferation and apoptosis. The other half of the cells was used to prepare whole cell lysates. Whole cell lysates from the 3 h and 24 h treatments were extracted and subjected to Western blots probed by anti-ac-tubulin or-β-actin antibody (panels A&B), or subjected to HDAC1 enzymatic assays post IP as described in the Materials and Methods (Panels C&D). The effects of the 3 h and 24 h HDACI treatments on cell proliferation, as reflected by percent decrease of live cells relative to untreated cells (panel E), and apoptosis (panel F) were determined by flow cytometry analysis as described in the Materials and Methods.

     

     

    PLoS One 2011 6, e17138. Mocetinostat (MGCD0103) purchased from Selleck.

  • Induction of DNA Damage and Bim Is Critical for HDACI-Induced Apoptosis in Pediatric AML Cells. THP-1 cells were treated with the HDACIs at Cmax concentrations for 3 (panel A) and 24 h (panel B), respectively. Whole cell lysates were extracted and subjected to Western blots probed by anti-p21, -c-Myc, -cH2AX, -Bim, or -b-actin antibody.

     

     

    PLoS One 2011 6, e17138. Mocetinostat (MGCD0103) purchased from Selleck.

    Western blot analysis of Acetyl-H3 and H3. 0-20μM MGCD0103 was added.

     

     

    Dr. Zhang of Tianjin Medical University. Mocetinostat (MGCD0103) 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 Mocetinostat (MGCD0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Phase 2.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC11 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC4 [1]
(Cell-free assay)
0.15 μM 0.29 μM 0.59 μM 1.66 μM >10 μM
In vitro

MGCD0103 inhibits only a subset of the nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11 at nanomolar or low micromolar concentrations, in a dose-dependent manner. MGCD0103 reveals most potent inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro, and it does not inhibit class II HDACs. The exocyclic amino group in MGCD0103 is necessary for enzyme inhibitory activity because HDAC-inhibitory activity against HDAC1 and HDAC2 is completely abolished with the desamino analogue. The inhibitory activity of MGCD0103 reaches the maximum plateau at 6 μM, and the maximal inhibitable enzyme pool affected by MGCD0103 is 75% of the total enzyme activity in HCT116 cells whereas NVP-LAQ824 inhibits almost 100% of that in these cells. In A549 cells, MGCD0103 also exhibits dose-dependent inhibition of HDAC activity in whole cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 M4XOPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\yZlQ5KGh? NGfQVJJKSzVyPUOuNFQh|ryP MWWyOlM4QDB|OB?=
BT549 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T1fFQ5KGh? MYTJR|UxRTRwM{ig{txO NYi4Wot1OjZ|N{iwN|g>
MCF7 Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H4U|Q5KGh? NXG1bY5bUUN3ME2wMlY4KM7:TR?= NWr2XlFSOjZ|N{iwN|g>
T47D MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzQS3I1QCCq NFPnb21KSzVyPUGuNVch|ryP M{XNT|I3Ozd6MEO4
MOLP8 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYm2OlNbPDhiaB?= Mmf2TWM2OD1yLkdCtUAxNjB2zszN NVrwW4N6OjZyOUG1NVg>
Panc1 NEj3c4xHfW6ldHnvckBCe3OjeR?= M3\aZlAvPS9zL{KuOUDPxE1? NUHyZ4dJPDhiaB?= NEj4dG5FVVOR MkKzeZBz\We3bHH0[ZMhdWmULUKwNy=> M2r4SVI2QDd{OUSx
Panc1 MnXtSpVv[3Srb36gRZN{[Xl? MnTKNE42NzFxMj61JO69VQ>? NIDJdZM1QCCq NFLwOYJFVVOR MmW5doVlfWOnczDlfJBz\XO|aX;uJI9nKFqHQkGgc44h[m:2aDDtVm5CKGGwZDDwdo91\WmwIHzleoVtyqB? NX3rUFlIOjV6N{K5OFE>
Panc1 NXnnO254SXCxcITvd4l{KEG|c3H5 M3f4PFHDqM7:TR?= MV[3NuKhcA>? MX3EUXNQ M4rTUJNmdnOrdHn6[ZMhWGGwY{GgZ4VtdHNiZn;yJIdmdWOrdHHibY5mNWmwZIXj[YQh[XCxcITvd4l{ NXT6Upc6OjV6N{K5OFE>
Panc1 NGfwXXNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXuxxsDPxE1? NIHxOY44OsLiaB?= NFXBR|hFVVOR M4[ycIVvcGGwY3XzJIdmdWOrdHHibY5mNWmwZIXj[ZMh[2WubDD2bYFjcWyrdImg[IVkemWjc3W= M1rsN|I2QDd{OUSx
MMCs NH;JfVhHfW6ldHnvckBCe3OjeR?= NYjvUIs{OSEQvH2= MkPNNE01QCCq NFv3T4pqdmO{ZXHz[ZMhVlCUQTDwdo91\WmwIHX4dJJme3Orb39CpFIvP+LCk{OuOUBnd2ym MXKyOFQ2OTN5OB?=
MMCs NFTHPHJHfW6ldHnvckBCe3OjeR?= NGTXZXoxNjVxMTFOwG0> MYeyOEBp NEThdYl{cG:5czC0OU1nd2ymIIP0bY12dGG2aX;uJIlvKGOJTWCgcIV3\Wy| MYeyOFQ2OTN5OB?=
MMCs MYXGeY5kfGmxbjDBd5NigQ>? M2e2SFHDqM7:TR?= MkDhNlQhcA>? MmfPbY5kemWjc3XzJGhCXCCjY4Tpeol1gQ>? M1\OUlI1PDVzM{e4
MMCs NXf5VldPTnWwY4Tpc44hSXO|YYm= M17SOlHDqM7:TR?= NGPDd5ozPCCq NFzDbHFifWevZX70d{BodG:kYXygZYNmfHmuYYTpc44hdGW4ZXzzJI9nKGirc4TvcoUhUDNvS{mvNVQhMEh|LVu5M|E1[WNrIHHu[EBJPC2NMUKgLGg1NUtzMnHjLS=> M{OweVI1PDVzM{e4
MMCs MWXGeY5kfGmxbjDBd5NigQ>? MYCxxsDPxE1? MYi2MVI1KGh? NYTvRoJ5\G:|ZT3k[ZBmdmSnboTsfUBqdmirYnn0d{B1cGVidILpcYV1cHmuYYTpc44hdGW4ZXygc4YhUDNvS{mgLGg{NUt7bXWzLS=> M4qwXVI1PDVzM{e4
BxPC-3 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7HSWM2OD1zLkGg{txO M1fOUFIyOzd3Nke5
AsPC-1 NFWyPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULSUJliTUN3ME2zMlkh|ryP NYrXd|VFOjF|N{W2O|k>
MiaPaca-2 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD4PGkxTUN3ME2wMlYh|ryP NFOwPXEzOTN5NU[3PS=>
Panc-1 NVfFb4VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvFR|UxRTFwODFOwG0> MkK1NlE{PzV4N{m=
PAXF 546L† NHX5UHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPjV2FGSzVyPUGuOUDPxE1? MXiyNVM4PTZ5OR?=
PAXF 1657L† MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;FR|UxRTBwMzFOwG0> MXiyNVM4PTZ5OR?=
HCT15 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNzFOwG0> MVqyNVMyPzR3NR?=
HT-29 NVznPWQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\OTWM2OD1yLkeg{txO MojDNlE{OTd2NUW=
SW48 NYji[mhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyTWM2OD1yLkig{txO NVLLemR[OjF|MUe0OVU>
SW620 NXjoem5ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnlZ4xKSzVyPUGg{txO NHTZR2kzOTNzN{S1OS=>
HMEC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTF7IN88US=> M3jTeFIyOzF5NEW1
ANBL6  Ml3nSpVv[3Srb36gRZN{[Xl? MnGxNeKh|ryP NYfwXXJYOjRiaB?= MkjN[Y5p[W6lZYOgOU1CSy2rbnT1Z4VlKE2DR1WtRVMh\2WwZTDlfJBz\XO|aX;u MX:yNVE4OTh{MR?=
LP1 MXfGeY5kfGmxbjDBd5NigQ>? M{DKVFHDqM7:TR?= NWW3O2h1OjRiaB?= NH;NeVlmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> NWLwO4RuOjFzN{G4NlE>
HD-LM2 MonLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrrWXY4OsLiaB?= M1HRfWROW09? MYDJR|UxRTFwOEig{txO M4X4b|IxQDhyMUC3
L428 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj5VmM4OsLiaB?= M1vpTmROW09? M4O3[2lEPTB;MT65OkDPxE1? MmLwNlA5QDBzMEe=
KM-H2 NGLSPYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;1NVM4OsLiaB?= NV\YZmhiTE2VTx?= MmHXTWM2OD1{Lki2JO69VQ>? MmrJNlA5QDBzMEe=
HD-LM2 NVPqNnI4TnWwY4Tpc44hSXO|YYm= MlTsNE4yNTJizszN MX2yOEBpyqB? NXKyW3hGTE2VTx?= NYLzVG17e2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> NHXwV5IzODh6MEGwOy=>
L428 NWj5cI1TTnWwY4Tpc44hSXO|YYm= MmnWNE4yNTJizszN M4nRbVI1KGkEoB?= M37McWROW09? M{P0V5Npd3e|IHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhOyCjbnSgeZBz\We3bHH0bY9vKG:oIITo[UBk\WyuIHP5Z4xmKHKnZ4XsZZRwenlicILveIVqdiCyMkG= NWfHTld1OjB6OECxNFc>
KM-H2 MmewSpVv[3Srb36gRZN{[Xl? M4D6R|AvOS1{IN88US=> NHLWeZMzPCCqwrC= MmrWSG1UVw>? NFjDVmN{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx MWGyNFg5ODFyNx?=
HD-LM2 MVXBdI9xfG:|aYOgRZN{[Xl? MUWwMlEwOC53L{Gg{txO MYW0PEBp NXjWOWFQTE2VTx?= MWHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NEjSfY0zODh6MEGwOy=>
L428 Mn;CRZBweHSxc3nzJGF{e2G7 NVTa[|JuOC5zL{CuOU8yKM7:TR?= MVe0PEBp MWDEUXNQ MofnbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MYmyNFg5ODFyNx?=
KM-H2 NXjBeIVNSXCxcITvd4l{KEG|c3H5 MnPzNE4yNzBwNT:xJO69VQ>? MkDaOFghcA>? MYLEUXNQ NVK4WIFJcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NGrvbIIzODh6MEGwOy=>
HD-LM2 MUHGeY5kfGmxbjDBd5NigQ>? NU[0NmVbOcLizszN Mn3WNlQwPDhiaB?= NEC4WolFVVOR M3[4ZYRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> NIrvdIozODh6MEGwOy=>
L428 M3\SeGZ2dmO2aX;uJGF{e2G7 NWi5SHRlOcLizszN M17yfVI1NzR6IHi= NVTMUZJoTE2VTx?= MkTL[I94dnKnZ4XsZZRmeyC[SVHQMEBi[3SrdnH0[YQh[2G|cHHz[ZMhQSCjbnSgNy=> NUPIXGx2OjB6OECxNFc>
KM-H2 M1riO2Z2dmO2aX;uJGF{e2G7 MWixxsDPxE1? NI\2UlAzPC92ODDo NE\QSG5FVVOR M4XseIRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> Mn\qNlA5QDBzMEe=
HD-LM2 MV\GeY5kfGmxbjDBd5NigQ>? MmnoNE42NzFizszN MUWyOE81QCCq NEm5UYlFVVOR NHzMZVl2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MX:yNFg5ODFyNx?=
L428 MVfGeY5kfGmxbjDBd5NigQ>? NWXHNHBjOC53L{Gg{txO MYOyOE81QCCq MVTEUXNQ Mn7meZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= M2PRRVIxQDhyMUC3
KM-H2 NHrIS2ZHfW6ldHnvckBCe3OjeR?= M4LFc|AvPS9zIN88US=> MkHENlQwPDhiaB?= MlzRSG1UVw>? M1XsZ5VxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 Mny1NlA5QDBzMEe=
HD-LM2 NETub3NHfW6ldHnvckBCe3OjeR?= MmjVNeKh|ryP NHfad2QxNjJ3LUS4JIg> NEnnRolFVVOR MXrhZ5RqfmG2ZYOgUmYuc0J? NGj2NnQzODh6MEGwOy=>
L428 MkjxSpVv[3Srb36gRZN{[Xl? MkXGNeKh|ryP M{TwW|AvOjVvNEigbC=> MUnEUXNQ MmnjZYN1cX[jdHXzJG5HNWuE MVeyNFg5ODFyNx?=
KM-H2 MUPGeY5kfGmxbjDBd5NigQ>? MlLRNeKh|ryP NGXyd5IxNjJ3LUS4JIg> M2X2emROW09? MmDCZYN1cX[jdHXzJG5HNWuE M17mcFIxQDhyMUC3
H526 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;ofolNUUN3ME20PFAhdk1? MXmyNFY5OjZ2Mx?=
H146 M{O0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUCyXoZiUUN3ME2zOUBvVQ>? NWnGR|A4OjB4OEK2OFM>
H82 NVfk[21KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLpTWM2OD1{NUCgcm0> NGXlZnkzODZ6Mk[0Ny=>
DMS114 NVTIWI9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnmTWM2OD14NECgcm0> M3LPSFIxPjh{NkSz
HeLa MoOySpVv[3Srb36gRZN{[Xl? Mmi4NE4{NTFyIN88US=> MnLrPEBp MlzESG1UVw>? NXK0N49KcW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT|khMEh|S{nBZ{kh[XRiMUCg{txO MVSyNFU{QDh2MB?=
HeLa MYnGeY5kfGmxbjDBd5NigQ>? MVmwMlMuOTBizszN NYDpPHNCQCCq M1jOdmROW09? NHnuN5ZqdmO{ZXHz[ZMh[2G|cHHz[UA{KGGwZDC3JIFkfGm4YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NX\kcXg5OjB3M{i4OFA>
HeLa NWnXR|RCTnWwY4Tpc44hSXO|YYm= MUCxNEDPxE4EoB?= NGjxV203NzF{L{K0JIg> MlPnSG1UVw>? M2PSO4lv\HWlZYOgcYl1d3SrYzDhZ4N2dXWuYYTpc44h[W6mIHTlcIF6\WRicEKxJIV5eHKnc4Ppc44> MlTYNlA2Ozh6NEC=
HeLa  MmnDSpVv[3Srb36gRZN{[Xl? NF\FbZoyOCEQvF5CpC=> NXPDe5I4PyCq NVLlVpZsTE2VTx?= NETwWYJlcXO{dYD0d{Bvd3KvYXygd5BqdmSuZTDjbIVkc3CxaX70JIZ2dmO2aX;u M3vGOlIxPTN6OESw
PBMC  NWTsXIJESXCxcITvd4l{KEG|c3H5 MnXwNE42NzJxMzFOwG0> NIXBNI4zPC92ODDo Ml3LbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M2HO[|IxPDB4OUS3

... Click to View More Cell Line Experimental Data

In vivo MGCD0103 significantly inhibites growth of human tumor xenografts in nude mice and the antitumor activity correlated with induction of histone acetylation in tumors. P.O. administration of MGCD0103 (2HBr salt) significantly decreases growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. MGCD0103 (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blockes growth of tumors compared with vehicle treatment alone with no change in body weight. In addition, MGCD0103 does not reduce WBC counts and is well tolerated. MGCD0103 is also orally active in many other human tumor xenograft models including NSCLC H1437. MGCD0103 at 80 mg/kg (free base) almost completely blocks the growth of H1437 tumors after 13 days of daily p.o. administration with no reduction of body weight in animals. [1] MGCD0103 reduces pulmonary arterial pressure more dramatically than tadalafil, a standard-of-care therapy for human pulmonary hypertension that functions as a vasodilator. Moreover, MGCD0103 improves pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope, which suggests a positive impact of the HDAC inhibitor on pulmonary vascular remodeling and stiffening. [2]

Protocol

Kinase Assay
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HDAC enzyme assay in vitro:

The deacetylase enzyme assay is based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes are incubated with MGCD0103 diluted in various concentrations for 10 minutes in assay buffer [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl2, 2.7 mM KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC is added to the reaction for further incubation at 37 °C. The concentration of the substrate and the incubation time varies for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allows the release of the fluorophore from the deacetylated substrate. The fluorescent signal is detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm.
Cell Research
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  • Cell lines: Human mammary epithelial cells (HMEC), human foreskin fibroblasts (MRHF) cells
  • Concentrations: 0-60 μM
  • Incubation Time: 72 hours
  • Method: Human mammary epithelial cells (HMEC) and human foreskin fibroblasts (MRHF) cells in 96-well plates are incubated with MGCD0103 at various concentrations for 72 hours at 37 °C in 5% CO2. MTT is added at a final concentration of 0.5 mg/ml and incubated with the cells for 4 hours before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] is added. After overnight incubation, solubilized dye is quantified by reading at 570 nm using a reference at 630 nm. Absorbance values are converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduces cell numbers to 50% relative to DMSO-treated cells is determined as MTT IC5
    (Only for Reference)
Animal Research
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  • Animal Models: Female CD-1 nude mice bearing H1437 tumors
  • Formulation: PBS acidified with 0.1 M HCl or PEG400/0.2 M HCl saline, 40:60
  • Dosages: 80 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (32.79 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 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 396.44
Formula

C23H20N6O

CAS No. 726169-73-9
Storage powder
in solvent
Synonyms MG0103

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02805660 Recruiting Advanced Cancer Mirati Therapeutics Inc. May 2016 Phase 1|Phase 2
NCT02303262 Recruiting Metastatic Leiomyosarcoma Sarcoma Alliance for Research through Collaboration September 2015 Phase 2
NCT02429375 Recruiting Hodgkin Lymphoma Memorial Sloan Kettering Cancer Center|MethylGene Inc. April 2015 Phase 1|Phase 2
NCT02236195 Active, not recruiting Urothelial Carcinoma Mirati Therapeutics Inc. October 2014 Phase 2
NCT02282358 Recruiting Lymphoma|Relapsed and Refractory|Diffuse Large B-Cell Lymphoma and Follicular Lymphoma Memorial Sloan Kettering Cancer Center|MethylGene Inc. October 2014 Phase 1|Phase 2
NCT02018926 Completed Myelodysplastic Syndrome Mirati Therapeutics Inc. December 2013 Phase 1|Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID