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Mocetinostat (MGCD0103)

Name: Mocetinostat (MGCD0103)
Brand: Selleck Chemicals
SKU: S1122
Rating: 5 (97 reviews)

Catalog No.S1122 Synonyms: MG0103

For research use only.

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.

Mocetinostat (MGCD0103) Chemical Structure

CAS No. 726169-73-9

Selleck's Mocetinostat (MGCD0103) has been cited by 97 publications

Purity & Quality Control

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HDAC Signaling Pathway Map

Biological Activity

Description

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	MliyRZBweHSxc3nzJGF{e2G7	NYHWO2NPOC53L{KvN{DPxE1?	NVO3[G1bOjRxNEigbC=>		NIniNHlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5	Ml3OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2ME[5OFcoRjJyNEC2PVQ4RC:jPh?=
HeLa	M3HrWWZ2dmO2aX;uJGF{e2G7	M{ezdVExKM7:TdMg	NEC3cJM4KGh?	NH:yOHZFVVOR	M4XKd4Rqe3K3cITzJI5wem2jbDDzdIlv\GynIHPo[YNseG:rboSg[pVv[3Srb36=	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV\|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa	MnjFSpVv[3Srb36gRZN{[Xl?	M3XwU\|ExKM7:TdMg	MVG2M\|EzNzJ2IHi=	M4PQVGROW09?	M1Xvd4lv\HWlZYOgcYl1d3SrYzDhZ4N2dXWuYYTpc44h[W6mIHTlcIF6\WRicEKxJIV5eHKnc4Ppc44>	NYDLepBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N\|g5PDBpPkKwOVM5QDRyPD;hQi=>
HeLa	MVfGeY5kfGmxbjDBd5NigQ>?	M3PjUVAvOy1zMDFOwG0>	M4i4dFghcA>?	NV3VSZhkTE2VTx?=	MnrTbY5kemWjc3XzJINie3Cjc3WgN{BidmRiNzDhZ5RqfmG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV\|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa	MlvMSpVv[3Srb36gRZN{[Xl?	M3jkblAvOy1zMDFOwG0>	NVi5cHlbQCCq	M{PuNWROW09?	NWPrfIpXcW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT\|khMEh\|S{nBZ{kh[XRiMUCg{txO	NF25PIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N\|g5PDB:L3G+
DMS114	Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M{nScmlEPTB;NkSwJI5O	M1;OblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H82	Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NYi0PW1zUUN3ME2yOVAhdk1?	Mn7sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
H146	NFTtcnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NEfkeFdKSzVyPUO1JI5O	M{n0SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H526	NHfDTGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NIDSeVdKSzVyPUS4NEBvVQ>?	M1jBZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
KM-H2	M{PQTWZ2dmO2aX;uJGF{e2G7	M2XWUFHDqM7:TR?=	M{\3cVAvOjVvNEigbC=>	MV;EUXNQ	NXn4UGU6[WO2aY\heIV{KE6ILXvC	NYHPOoRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428	MVPGeY5kfGmxbjDBd5NigQ>?	NIK1V40yyqEQvF2=	NGC0WVMxNjJ3LUS4JIg>	NEmwTFhFVVOR	NInQcJRi[3SrdnH0[ZMhVkZva1K=	NEH6dXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2	NVnFeoR[TnWwY4Tpc44hSXO\|YYm=	MVyxxsDPxE1?	Mne1NE4zPS12ODDo	M2Gxc2ROW09?	NHTyOXdi[3SrdnH0[ZMhVkZva1K=	M3;MTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2	Ml;JSpVv[3Srb36gRZN{[Xl?	NYmxV2kyOC53L{Gg{txO	NEDUSoYzPC92ODDo	MVfEUXNQ	MnPteZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm=	Ml61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428	Mk\RSpVv[3Srb36gRZN{[Xl?	M{XuPFAvPS9zIN88US=>	MXKyOE81QCCq	MW\EUXNQ	M2LQZZVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5	MlTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2	MVrGeY5kfGmxbjDBd5NigQ>?	NFfJfpYxNjVxMTFOwG0>	MmTFNlQwPDhiaB?=	MY\EUXNQ	MlS3eZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm=	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2	MX\GeY5kfGmxbjDBd5NigQ>?	NFuxbHQyyqEQvF2=	NVfwW2xPOjRxNEigbC=>	MV3EUXNQ	NV2xTHNo\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>?	Mmq5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428	NEDKSmVHfW6ldHnvckBCe3OjeR?=	M3v0flHDqM7:TR?=	M2TLZ\|I1NzR6IHi=	M4iz[GROW09?	NYDzT2Jw\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>?	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2	MnToSpVv[3Srb36gRZN{[Xl?	NXTDVmRMOcLizszN	NXzGcng3OjRxNEigbC=>	NI\Bd2VFVVOR	NXHRVXdC\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>?	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2	NELVOm1CeG:ydH;zbZMhSXO\|YYm=	M3LxWFAvOS9yLkWvNUDPxE1?	MlPlOFghcA>?	M3;OWGROW09?	NWjQZZpMcW6mdXPld{BieG:ydH;zbZMh\G:\|ZTDk[ZBmdmSnboTsfS=>	NEnK[5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428	NFXXbINCeG:ydH;zbZMhSXO\|YYm=	M37WS\|AvOS9yLkWvNUDPxE1?	MYW0PEBp	M2frfGROW09?	NX7CcGxncW6mdXPld{BieG:ydH;zbZMh\G:\|ZTDk[ZBmdmSnboTsfS=>	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2	NWTYe\|BsSXCxcITvd4l{KEG\|c3H5	MoLzNE4yNzBwNT:xJO69VQ>?	MX[0PEBp	NHLZRmhFVVOR	NUjjZ2lPcW6mdXPld{BieG:ydH;zbZMh\G:\|ZTDk[ZBmdmSnboTsfS=>	NVf0Z2lrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2	NVTVbmxUTnWwY4Tpc44hSXO\|YYm=	NXjuSmtTOC5zLUKg{txO	MYiyOEBpyqB?	NGjZc5lFVVOR	M1THS5Npd3e\|IHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhOyCjbnSgeZBz\We3bHH0bY9vKG:oIITo[UBk\WyuIHP5Z4xmKHKnZ4XsZZRwenlicILveIVqdiCyMkG=	M4DD[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428	NXfuNHNRTnWwY4Tpc44hSXO\|YYm=	NYPySWVqOC5zLUKg{txO	M4LwNFI1KGkEoB?=	NImwUmVFVVOR	MUfzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz	NXPyboJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2	M1S2UmZ2dmO2aX;uJGF{e2G7	MkfPNE4yNTJizszN	M2nTTFI1KGkEoB?=	MonRSG1UVw>?	MnSxd4hwf3NiYXPleJlt[XSrb36gc4YhcGm\|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?=	M2G1[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M37BcVczyqCq	M1r6W2ROW09?	NFHLbW1KSzVyPUKuPFYh\|ryP	MojRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428	M3zrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXW3NuKhcA>?	NEXiS3FFVVOR	Mmr4TWM2OD1zLkm2JO69VQ>?	NX3tcHFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MUC3NuKhcA>?	M1PSW2ROW09?	NWT1TFFtUUN3ME2xMlg5KM7:TR?=	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
LP1	NWe2[JdwTnWwY4Tpc44hSXO\|YYm=	NV7t[WEyOcLizszN	M1y0T\|I1KGh?		M2fDXoVvcGGwY3XzJFUuSUNvaX7keYNm\CCPQVfFMWE{KGenbnWg[ZhxemW\|c3nvci=>	NX\sS484RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGxO\|E5OjFpPkKxNVcyQDJzPD;hQi=>
ANBL6	NUL4OlhETnWwY4Tpc44hSXO\|YYm=	Ml7SNeKh\|ryP	NVf4RWVOOjRiaB?=		NVfXRoFb\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF5MUiyNUc,OjFzN{G4NlE9N2F-
HMEC	M{nkeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NHTmVGRKSzVyPUG5JO69VQ>?	M1\wSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO\|Q2PTxxYU6=
SW620	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MUnJR\|UxRTFizszN	NELkWZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO\|Q2PSd-MkGzNVc1PTV:L3G+
SW48	M2K0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M2nPTWlEPTB;MD64JO69VQ>?	M{XwfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO\|Q2PTxxYU6=
HT-29	M3W5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NVzmdJpHUUN3ME2wMlch\|ryP	M1TLUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO\|Q2PTxxYU6=
HCT15	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M1fnSmlEPTB;MD63JO69VQ>?	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF\|MUe0OVU9N2F-
PAXF 1657L†	NVfCNHFJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NF3z[pVGSzVyPUCuN{DPxE1?	MkjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF\|N{W2O\|koRjJzM{e1Olc6RC:jPh?=
PAXF 546L†	M1nSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFHKeYJGSzVyPUGuOUDPxE1?	NYXWcI4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO\|U3PzlpPkKxN\|c2Pjd7PD;hQi=>
Panc-1	NXG0R5ZMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MoLMSWM2OD1zLkig{txO	MnHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF\|N{W2O\|koRjJzM{e1Olc6RC:jPh?=
MiaPaca-2	NH\6NnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MoD1SWM2OD1yLk[g{txO	NVj3XIxXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO\|U3PzlpPkKxN\|c2Pjd7PD;hQi=>
AsPC-1	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MnLwSWM2OD1\|Lkmg{txO	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF\|N{W2O\|k9N2F-
BxPC-3	NGG4[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NHnpPVBGSzVyPUGuNUDPxE1?	NIX5emU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3OVY4QSd-MkGzO\|U3Pzl:L3G+
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HeLa	NUj5cW5GTnWwY4Tpc44h[XO\|YYm=	MX[xJJRwKDFyIIXN	Mk\ZNlQhcHK\|		M2PzemlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBJ\UyjIHPlcIx{KGG\|c3Xzd4VlKGG\|IHnuZ5Jm[XOnIHnuJGg{UzmDYzDs[ZZmdCCjdDCxJJRwKDFyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	NHOxO409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyPVQ5Oyd-MkO4Nlk1QDN:L3G+
Jurkat	MnjzSpVv[3Srb36gZZN{[Xl?	M2TaSlEhfG9iMUCgeW0>	MWGyOEBpenN?		NH7uSHpKdmirYnn0bY9vKG:oIFjERWMhcW5iaIXtZY4hUnW{a3H0JINmdGy\|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKEh\|S{nBZ{Bt\X[nbDDheEAyKHSxIEGwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	NYXBS2Q3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4Nlk1QDNpPkKzPFI6PDh\|PD;hQi=>
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A673	NUfUVYcxeUiWUzDhd5NigQ>?				Mki1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	NF:1VlZyUFSVIHHzd4F6				NFXqXVJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=>	MoDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-37	NHG0fHByUFSVIHHzd4F6				MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN?	NYX2NJd1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
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NB1643	MWrxTHRUKGG\|c3H5				NEK4RlRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz	M3vtSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	MV3xTHRUKGG\|c3H5				MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	NGDHOXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
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SJ-GBM2	MVnxTHRUKGG\|c3H5				MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTTk1ISk1{IHPlcIx{	NXvJb2hxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
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HCT116	M37qemFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NHWxcYk4OiCqcoO=		M4DSfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVMvPTIQvF2=	NEi5eIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK\|5EcEWPQly8M4E,
HepG2	NVXyOHdISW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MUK0PEBpenN?		MmfRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME20MlA2\|ryP	MoPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HepG2	MYLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MkjzO\|IhcHK\|		MnH2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME20MlI2\|ryP	MojxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HepG2	MWjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		Mm\TNlQhcHK\|		MnqwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME21Mlc6\|ryP	MlPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
A549	NXL4NXdnSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{XwRlczKGi{cx?=		M{XGdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNU45P87:TR?=	MnHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
A549	MlHJRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MY[0PEBpenN?		M{PRUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOE42P87:TR?=	MlfIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HCT116	NVTuWmJYSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MYOyOEBpenN?		M2fDfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI6NjZ7zszN	MnXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HeLa	M33VfmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MkfjNlQhcHK\|		MlrQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZVzhJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUSzMljPxE1?	NUnodHlqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?

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 ; Ac-H3 / Ac-H4 / Ac-tubulin	27551526 29186204
Immunofluorescence	E-cadherin / ZEB1 ; Nanog / MHC	25872941 26240433
Growth inhibition assay	Cell viability	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 (from reference)

Kinase Assay:^[1]	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]	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
Animal Research:^[1]	Animal Models: Female CD-1 nude mice bearing H1437 tumors Dosages: 80 mg/kg Administration: Administered via p.o.

References

Solubility (25°C)

In vitro


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. Click to purchase: PEG400 Tween 80	30mg/mL

Chemical Information

Molecular Weight	396.44
Formula	C₂₃H₂₀N₆O
CAS No.	726169-73-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

Download Mocetinostat (MGCD0103) SDF

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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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