Mocetinostat (MGCD0103)

For research use only.

Catalog No.S1122 Synonyms: MG0103

90 publications

Mocetinostat (MGCD0103) Chemical Structure

CAS No. 726169-73-9

Mocetinostat (MGCD0103, MG0103) 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. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.

Selleck's Mocetinostat (MGCD0103) has been cited by 90 publications

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Mocetinostat (MGCD0103, MG0103) 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. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC11 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
0.15 μM 0.29 μM 0.59 μM 1.66 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
PBMC  MX;BdI9xfG:|aYOgRZN{[Xl? NUf6cFBjOC53L{KvN{DPxE1? M4i5N|I1NzR6IHi= M{HFcolv\HWlZYOgZZBweHSxc3nzJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NILWU489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MESwOlk1Pyd-MkC0NFY6PDd:L3G+
HeLa  NHTsVXJHfW6ldHnvckBCe3OjeR?= Mne4NVAh|ryPwrC= NUju[YlWPyCq NETVNZRFVVOR MoK1[Il{enWydIOgco9zdWGuIIPwbY5ldGViY3jlZ4txd2mwdDDmeY5kfGmxbh?= NHnxVXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N|g5PDB:L3G+
HeLa M3;QVWZ2dmO2aX;uJGF{e2G7 Ml3HNVAh|ryPwrC= Ml\vOk8yOi9{NDDo NUjpdIpXTE2VTx?= NHT5b5pqdmS3Y3XzJI1qfG:2aXOgZYNkfW23bHH0bY9vKGGwZDDk[YxigWWmIICyNUBmgHC{ZYPzbY9v MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa NF7VdnZHfW6ldHnvckBCe3OjeR?= MorwNE4{NTFyIN88US=> MYW4JIg> NYTLTY14TE2VTx?= M4rKdYlv[3KnYYPld{Bk[XOyYYPlJFMh[W6mIEegZYN1cX[jdHnvckBld3OnIHTldIVv\GWwdHz5 M4DSPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUO4PFQxLz5{MEWzPFg1ODxxYU6=
HeLa M4XWZmZ2dmO2aX;uJGF{e2G7 NFTkd5kxNjNvMUCg{txO NITBclA5KGh? NWPufJE1TE2VTx?= MlK2bY5kemWjc3XzJIFk\XS7bHH0[YQhUDNiS{mgLGg{UzmDYzmgZZQhOTBizszN NXe0NXJSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
DMS114 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DKPWlEPTB;NkSwJI5O MkK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
H82 NG\ibIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G4eWlEPTB;MkWwJI5O M3rOVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H146 NWm4T4djT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C4SGlEPTB;M{Wgcm0> MkD5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
H526 MnTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHxTWM2OD12OECgcm0> NHnsTXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[4NlY1Oyd-MkC2PFI3PDN:L3G+
KM-H2 NU[5Oo9XTnWwY4Tpc44hSXO|YYm= MoTENeKh|ryP NUfobo1vOC5{NT20PEBp M4HZNWROW09? MWDhZ5RqfmG2ZYOgUmYuc0J? NXKxV5N1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 NY\YWIVMTnWwY4Tpc44hSXO|YYm= NWTmU5NoOcLizszN NEjySGoxNjJ3LUS4JIg> MmLBSG1UVw>? NGHrWldi[3SrdnH0[ZMhVkZva1K= NUm3cYoyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 MV\GeY5kfGmxbjDBd5NigQ>? MoHGNeKh|ryP NELzeIgxNjJ3LUS4JIg> M1TDemROW09? M1zieIFkfGm4YYTld{BPTi2tQh?= NUS0e29HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 MV7GeY5kfGmxbjDBd5NigQ>? NXLmSoNnOC53L{Gg{txO MX6yOE81QCCq MV3EUXNQ Mn\qeZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MkDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 NGj2WW5HfW6ldHnvckBCe3OjeR?= NXOz[WE4OC53L{Gg{txO M4DXT|I1NzR6IHi= M4jGdGROW09? MmDkeZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NY\oW4ZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 MX7GeY5kfGmxbjDBd5NigQ>? NUHsbFdMOC53L{Gg{txO MmfXNlQwPDhiaB?= MnjESG1UVw>? M1HNbpVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NGLPVlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
KM-H2 M4f3ZmZ2dmO2aX;uJGF{e2G7 NFzyN2EyyqEQvF2= Mk\LNlQwPDhiaB?= M4L5bGROW09? NEHWVoZld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ Mn;kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 MkS1SpVv[3Srb36gRZN{[Xl? M{\yRVHDqM7:TR?= Mn\vNlQwPDhiaB?= MXnEUXNQ NYX6Slds\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? NXHS[IVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 M3nYV2Z2dmO2aX;uJGF{e2G7 MmfPNeKh|ryP NE\ke4szPC92ODDo NV\EWmlRTE2VTx?= NGmxbWtld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ MkXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
KM-H2 M2OzOWFxd3C2b4Ppd{BCe3OjeR?= NHyyW|cxNjFxMD61M|Eh|ryP NHvXbG81QCCq NGrSWWlFVVOR M3\YVYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
L428 MVLBdI9xfG:|aYOgRZN{[Xl? NFPxZ|IxNjFxMD61M|Eh|ryP NF\pcZI1QCCq Mn\NSG1UVw>? NFPWe2tqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M2PCR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2 MVjBdI9xfG:|aYOgRZN{[Xl? M4TaVVAvOS9yLkWvNUDPxE1? NEP6V2E1QCCq MlTRSG1UVw>? MV\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NVu0[XNbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 NFLabHNHfW6ldHnvckBCe3OjeR?= NWD6O2pDOC5zLUKg{txO MYqyOEBpyqB? Mme2SG1UVw>? NIG4NGx{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx Ml7SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 MmnaSpVv[3Srb36gRZN{[Xl? NULxO45bOC5zLUKg{txO MYGyOEBpyqB? MWPEUXNQ NGPwPZd{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx M2n2OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2 MV;GeY5kfGmxbjDBd5NigQ>? M4DDWVAvOS1{IN88US=> MlrtNlQhcMLi M1HTZ2ROW09? Mo\Ud4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= M3XMVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[1XXF6PzMEoHi= MkDMSG1UVw>? MmG5TWM2OD1{Lki2JO69VQ>? NWX2TmxVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 NWXFOGlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvxTVNPPzMEoHi= MXzEUXNQ MVrJR|UxRTFwOU[g{txO NUTjfJQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 NIGxWlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO3NuKhcA>? Mkf2SG1UVw>? NGPTV41KSzVyPUGuPFgh|ryP NHPoRYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
LP1 NW\0WVRbTnWwY4Tpc44hSXO|YYm= NEGxPYoyyqEQvF2= MofCNlQhcA>? MV\lcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= M{\CNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMUexPFIyLz5{MUG3NVgzOTxxYU6=
ANBL6  M2XZVWZ2dmO2aX;uJGF{e2G7 NFnnc4wyyqEQvF2= NEnBNnEzPCCq M1\jUoVvcGGwY3XzJFUuSUNvaX7keYNm\CCPQVfFMWE{KGenbnWg[ZhxemW|c3nvci=> Moi5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzN{G4NlEoRjJzMUexPFIyRC:jPh?=
HMEC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF7IN88US=> NGLCd2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
SW620 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDZO49GUUN3ME2xJO69VQ>? MmrDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
SW48 NEK5PXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIThSnhKSzVyPUCuPEDPxE1? NI\zOGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
HT-29 NHq1U4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwNzFOwG0> NIm0T3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
HCT15 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jn[GlEPTB;MD63JO69VQ>? Mmm0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
PAXF 1657L† NV7IS|FHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfDdHhrTUN3ME2wMlMh|ryP MlvtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{W2O|koRjJzM{e1Olc6RC:jPh?=
PAXF 546L† Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fpWGVEPTB;MT61JO69VQ>? M1;wO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
Panc-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PHZmVEPTB;MT64JO69VQ>? NH;Pcoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3OVY4QSd-MkGzO|U3Pzl:L3G+
MiaPaca-2 NVH2fY9PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe5d2RGSzVyPUCuOkDPxE1? NWHBTHVoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
AsPC-1 M1\oSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvFR|UxRTNwOTFOwG0> NHuyOnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3OVY4QSd-MkGzO|U3Pzl:L3G+
BxPC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjFR|UxRTFwMTFOwG0> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
MMCs MVPGeY5kfGmxbjDBd5NigQ>? NGfrSW4yyqEQvF2= M4TDSlYuOjRiaB?= NHX0OG5ld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTzJJRp\SC2cnnt[ZRpgWyjdHnvckBt\X[nbDDv[kBJOy2NOTCoTFMuUzmvZUOp M3XzZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxN|c5Lz5{NES1NVM4QDxxYU6=
MMCs NF7TcVVHfW6ldHnvckBCe3OjeR?= M2PDXFHDqM7:TR?= MYqyOEBp M3nTN4F2\22nboTzJIdtd2KjbDDhZ4V1gWyjdHnvckBt\X[nbIOgc4YhcGm|dH;u[UBJOy2NOT:xOEApUDNvS{mvNVRi[yliYX7kJGg1NUtzMjCoTFQuUzF{YXOp M2nKbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxN|c5Lz5{NES1NVM4QDxxYU6=
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A549 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoLSO|IhcHK| MkTORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGxMlg4|ryP MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|I6QDBxJ{7DbGVOSkx:L3G+
A549 NH\TSXJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NIWwfoI1QCCqcoO= M4XrcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOE42P87:TR?= NFvweWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK|5EcEWPQly8M4E,
HCT116 NInzTIxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NH\Ud2szPCCqcoO= NUHsVIRHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDJ2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OjlwNkpOwG0> Ml7rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HeLa MoL3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MknlNlQhcHK| NVG2N4xGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQ{NjkQvF2= NFjlTGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK|5EcEWPQly8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Bad / Bid / Bak / Puma / Bax / Cleaved caspase-9 / Cleaved caspase-3 / Cleaved PARP; 

PubMed: 27551526     


(a and b) DU-145 cells were treated with various doses of mocetinostat for 24 h. Western blotting was performed using the indicated antibodies. 

Ac-H3 / Ac-H4 / Ac-tubulin ; 

PubMed: 29186204     


Mocetinostat increased acetylated histone 3 and 4 in a time- and dose-dependent manner in LMS cells. Mocetinostat did not increase acetylated tubulin expression.

27551526 29186204
Immunofluorescence
E-cadherin / ZEB1 ; 

PubMed: 25872941     


Immunoblot and immunofluorescence showing that mocetinostat treatment (1 μM, 48 h) reduced ZEB1 expression and induced E-cadherin in Panc1. Expression of histone deacetylases was not altered by mocetinostat, but histone acetylation was induced. Scale bar 10 μm.

Nanog / MHC ; 

PubMed: 26240433     


c-Kit+ cells were treated with 2 µM MOCE for 2 or 7 days, as indicated. The cells were double-labeled with anti-Nanog (green) and anti-αMHC (red) antibodies. Nuclei were stained with DAPI (blue). The upper right section of each panel shows the enlargement of the box-selected area. Scale bars = 20 µm.

25872941 26240433
Growth inhibition assay
Cell viability; 

PubMed: 26378038     


B. Cells were treated with increasing concentrations of mocetinostat for 48 hours and assayed by the WST-1 cell viability assay. C. IC50 values were calculated by the GraphPad Prism software. 

26378038
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:[1]
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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:[1]
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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:[1]
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  • Animal Models: Female CD-1 nude mice bearing H1437 tumors
  • 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.
30mg/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 396.44
Formula

C23H20N6O

CAS No. 726169-73-9
Storage powder
in solvent
Synonyms MG0103
Smiles C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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 SDS / 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04299113 Recruiting Drug: Vinorelbine|Drug: Mocetinostat Rhabdomyosarcoma Jonsson Comprehensive Cancer Center|Mirati Therapeutics Inc.|Phase One Foundation May 14 2020 Phase 1
NCT02993991 Withdrawn Drug: Mocetinostat|Biological: Durvalumab Squamous Cell Carcinoma Head And Neck|Squamous Cell Carcinoma Mouth|Resectable Squamous Cell Carcinoma of Oral Cavity University Health Network Toronto|Mirati Therapeutics Inc.|AstraZeneca October 10 2017 Phase 1
NCT02236195 Completed Drug: Mocetinostat Urothelial Carcinoma Mirati Therapeutics Inc. October 2014 Phase 2
NCT00666497 Terminated Drug: Azacitidine|Drug: MGCD0103 Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS) Mirati Therapeutics Inc. June 2008 Phase 2
NCT00511576 Terminated Drug: MGCD0103 & Docetaxel Breast Cancer|Lung Cancer|Pulmonary Cancer|Non-Small-Cell Lung Carcinoma|Prostate Cancer|Prostatic Cancer|Gastric Cancer|Stomach Cancer Mirati Therapeutics Inc. August 2007 Phase 1

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