Mocetinostat (MGCD0103)

Name: Mocetinostat (MGCD0103)
Brand: Selleck Chemicals
SKU: S1122
Rating: 5 (86 reviews)

For research use only.

Catalog No.S1122 Synonyms: MG0103

86 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 86 publications

Cancer Cell, 2021, S1535-6108(20)30662-0

PubMed: 33482121 ( click the link to review the publication )

Cancer Cell, 2016, 29(3):311-323

PubMed: 26977882 ( click the link to review the publication )

Nat Biotechnol, 2015, 10.1038/nbt.3130

PubMed: 25751058 ( click the link to review the publication )

Cancer Discov, 2020, CD-20-0336

PubMed: 32978226 ( click the link to review the publication )

Sci Rep, 2020, 10(1):4337

PubMed: 32152395 ( click the link to review the publication )

Front Genet, 2020, 11:80

PubMed: 32158467 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 8:752

PubMed: 32850856 ( click the link to review the publication )

Biomed Res Int, 2020, 2020:4705615

PubMed: 32775424 ( click the link to review the publication )

Cancer Sci, 2020, 111(7):2374-2384

PubMed: 32391602 ( click the link to review the publication )

Acta Pharm Sin B, 2020, 10(4):615-627

PubMed: 32322466 ( click the link to review the publication )

J Cancer, 2020, 11(7):1915-1926

PubMed: 32194803 ( click the link to review the publication )

Cell Syst, 2019, 8(2):97-108

PubMed: 30797775 ( click the link to review the publication )

J Immunother Cancer, 2019, 7(1):33

PubMed: 30728070 ( click the link to review the publication )

Cancer Discov, 2019, 9(4):526-545

PubMed: 30709805 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(1):185-195

PubMed: 30301863 ( click the link to review the publication )

Mol Oncol, 2019, 13(9):1944-1958

PubMed: 31225930 ( click the link to review the publication )

Pharmacol Res, 2019, 146:104281

PubMed: 31125601 ( click the link to review the publication )

ACS Omega, 2019, 4(22):19895-19904

PubMed: 31788622 ( click the link to review the publication )

Commun Biol, 2019, 2:272

PubMed: 31372511 ( click the link to review the publication )

EMBO Rep, 2018, 19(9)

PubMed: 30021835 ( click the link to review the publication )

Cancer Res, 2018, 78(20):5731-5740

PubMed: 30135193 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(2):381-392

PubMed: 28839000 ( click the link to review the publication )

J Virol, 2018, 92(6)

PubMed: 29298886 ( click the link to review the publication )

JCI Insight, 2018, 3(22)125568

PubMed: 30429379 ( click the link to review the publication )
Curr Protoc Pharmacol, 2018, 81(1):e41

PubMed: 29927058 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(11):6334-6349

PubMed: 28369619 ( click the link to review the publication )

Oncogene, 2017, 36(12):1707-1720

PubMed: 27694895 ( click the link to review the publication )

J Mol Cell Cardiol, 2017, 112:74-82

PubMed: 28886967 ( click the link to review the publication )

Biotechnol Bioeng, 2017, 114(11):2660-2667

PubMed: 28667749 ( click the link to review the publication )

J Pharmacol Exp Ther, 2017, 361(1):140-150

PubMed: 28174211 ( click the link to review the publication )

Pain Physician, 2017, 20(5):E673-E685

PubMed: 28727712 ( click the link to review the publication )

Theriogenology, 2017, 87:298-305

PubMed: 27742403 ( click the link to review the publication )

Circ J, 2017, 82(1):192-202

PubMed: 28747611 ( click the link to review the publication )

JCI Insight, 2017, 2(6):e90196

PubMed: 28352655 ( click the link to review the publication )

Oncotarget, 2017, 8(4):6319-6329

PubMed: 28030834 ( click the link to review the publication )

Cell Death Discov, 2016, 2:16036

PubMed: 27551526 ( click the link to review the publication )

Mol Oncol, 2016, 10(5):735-750

PubMed: 26775640 ( click the link to review the publication )

ACS Chem Biol, 2016, 11(10):2685-2692

PubMed: 27459069 ( click the link to review the publication )

J Lipid Res, 2016, 57(5):868-81

PubMed: 27013100 ( click the link to review the publication )

Sci Rep, 2016, 6:38407

PubMed: 27910927 ( click the link to review the publication )

Am J Physiol Lung Cell Mol Physiol, 2016, 311(1):L124-34

PubMed: 27233998 ( click the link to review the publication )

J Biol Chem, 2016, 291(16):8745-55

PubMed: 26912657 ( click the link to review the publication )

Mol Cell Biol, 2016, 36(22):2838-2854

PubMed: 27573019 ( click the link to review the publication )

Future Med Chem, 2016, 8(13):1553-71

PubMed: 26971619 ( click the link to review the publication )

Cell Signal, 2016, 28(8):1015-24

PubMed: 27185186 ( click the link to review the publication )

Hypertens Res, 2016, 39(10):709-716

PubMed: 27278287 ( click the link to review the publication )

Nat Commun, 2015, 3;6:10091

PubMed: 26631872 ( click the link to review the publication )

Nucleic Acids Res, 2015, 10.1093/nar/gkv188

PubMed: 25769527 ( click the link to review the publication )
Mol Cancer Ther, 2015, 14(4):1014-23

PubMed: 25673820 ( click the link to review the publication )

Mol Oncol, 2015, 9(7):1447-1457

PubMed: 25957812 ( click the link to review the publication )

FEBS Lett, 2015, 589(10):1080-8

PubMed: 25816750 ( click the link to review the publication )

Sheng Li Xue Bao, 2015, 67(5):447-54

PubMed: 26490061 ( click the link to review the publication )

Oncotarget, 2015, 6(28):25784-800

PubMed: 26329759 ( click the link to review the publication )

Oncotarget, 2015, 6(32):33623-35

PubMed: 26378038 ( click the link to review the publication )

Oncotarget, 2015, 6(24):20449-65

PubMed: 26036259 ( click the link to review the publication )

Cancer Immunol Res, 2015, 3(12):1375-85

PubMed: 26297712 ( click the link to review the publication )

Western University, 2015, Western University

PubMed: ( click the link to review the publication )

Blood, 2014, 123(10):1535-43

PubMed: 24449212 ( click the link to review the publication )

J Heart Lung Transplant, 2014, 33(6):644-53

PubMed: 24746638 ( click the link to review the publication )

PLoS Pathog, 2014, 10(4):e1004071

PubMed: 24722454 ( click the link to review the publication )

J Neurosci, 2014, 34(17):6112-22

PubMed: 24760871 ( click the link to review the publication )

BMC Biol, 2014, 12:95

PubMed: 25406762 ( click the link to review the publication )

BMC Biol, 2014, 10.1186/1741-7007-12-30

PubMed: 24779377 ( click the link to review the publication )

Oncogenesis, 2014, 3:e127

PubMed: 25402609 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2014, 274(1):7-17

PubMed: 24200994 ( click the link to review the publication )

Cell Signal, 2014, 26(12):2912-20

PubMed: 25220405 ( click the link to review the publication )

Assay Drug Dev Technol, 2014, 12(9-10):514-26

PubMed: 25506801 ( click the link to review the publication )

Fibrogenesis Tissue Repair, 2014, 7:10

PubMed: 25024745 ( click the link to review the publication )

Mol Cell, 2013, 52(3):406-20

PubMed: 24120667 ( click the link to review the publication )

Nat Struct Mol Biol, 2013, 20(3):317-25

PubMed: 23377543 ( click the link to review the publication )

Nat Commun, 2013, 4:2735

PubMed: 24193185 ( click the link to review the publication )

Oncogene, 2013, 33(5):653-64

PubMed: 23524580 ( click the link to review the publication )
J Neurosci, 2013, 33(17):7535-47

PubMed: 23616558 ( click the link to review the publication )

Pain, 2013, 154(9):1668-79

PubMed: 23693161 ( click the link to review the publication )

J Dent Res, 2013, 93(2):148-54

PubMed: 24334408 ( click the link to review the publication )

Mol Pharm, 2013, 10(1):307-18

PubMed: 23186311 ( click the link to review the publication )

J Am Heart Assoc, 2013, 2(5):e000317

PubMed: 24088507 ( click the link to review the publication )

Melanoma Res, 2013, 23(5):341-8

PubMed: 23963286 ( click the link to review the publication )

J Thromb Thrombolysis, 2013, 35(2):185-92

PubMed: 23229086 ( click the link to review the publication )

Circ Res, 2012, 110(5):739-48

PubMed: 22282194 ( click the link to review the publication )

Oncogene, 2012, 32(33):3896-903

PubMed: 22945647 ( click the link to review the publication )

Biochem J, 2012, 447(3):457-64

PubMed: 22908849 ( click the link to review the publication )

PLoS One, 2012, 7(12):e52095

PubMed: 23251689 ( click the link to review the publication )

Oncogene, 2011, 30(27):3062-72

PubMed: 21577204 ( click the link to review the publication )

J Biol Chem, 2011, 286(27):23842-51

PubMed: 21489983 ( click the link to review the publication )

PLoS One, 2011, 6(2):e17138

PubMed: 21359182 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HDAC Inhibitors

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	NV\DTJVGSXCxcITvd4l{KEG\|c3H5	MUKwMlUwOi9\|IN88US=>	MnHxNlQwPDhiaB?=		M{\Sb4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODRyNkm0O{c,OjB2ME[5OFc9N2F-
HeLa	NIrufZBHfW6ldHnvckBCe3OjeR?=	NUj6VFltOTBizszNxsA>	NFfJ[4g4KGh?	M4W1Z2ROW09?	NVnFflB1\Gm\|coXweJMhdm:{bXHsJJNxcW6mbHWgZ4hm[2uyb3nueEBnfW6ldHnvci=>	MojGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3M{i4OFAoRjJyNUO4PFQxRC:jPh?=
HeLa	MoDnSpVv[3Srb36gRZN{[Xl?	NE\VdXIyOCEQvF5CpC=>	NG\Dfos3NzF{L{K0JIg>	NUPyRmYxTE2VTx?=	MV\pcoR2[2W\|IH3peI91cWNiYXPjeY12dGG2aX;uJIFv\CCmZXzhfYVlKHB{MTDlfJBz\XO\|aX;u	NWfXdFQyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N\|g5PDBpPkKwOVM5QDRyPD;hQi=>
HeLa	MkjuSpVv[3Srb36gRZN{[Xl?	MXewMlMuOTBizszN	NUHqfZRuQCCq	MXPEUXNQ	MlLlbY5kemWjc3XzJINie3Cjc3WgN{BidmRiNzDhZ5RqfmG2aX;uJIRwe2ViZHXw[Y5l\W62bIm=	NFXPTo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N\|g5PDB:L3G+
HeLa	M2PyN2Z2dmO2aX;uJGF{e2G7	MmPBNE4{NTFyIN88US=>	MUi4JIg>	NWfLcZV[TE2VTx?=	NIHvcmRqdmO{ZXHz[ZMh[WOndInsZZRm\CCKMzDLPUApUDONOVHjLUBifCBzMDFOwG0>	MmrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3M{i4OFAoRjJyNUO4PFQxRC:jPh?=
DMS114	M1OyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MVTJR\|UxRTZ2MDDuUS=>	NIPmWHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[4NlY1Oyd-MkC2PFI3PDN:L3G+
H82	M{jPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NV\JWoM3UUN3ME2yOVAhdk1?	M2P6XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H146	MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Mkm5TWM2OD1\|NTDuUS=>	NWrsbZR2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFI3PDNpPkKwOlgzPjR\|PD;hQi=>
H526	NWrlRlNoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVHJR\|UxRTR6MDDuUS=>	M4GwNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
KM-H2	NGn0U3VHfW6ldHnvckBCe3OjeR?=	NY\uV2ZjOcLizszN	Mn71NE4zPS12ODDo	NH3r[5lFVVOR	NHjwZmxi[3SrdnH0[ZMhVkZva1K=	NFfEdXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428	NX7ZS3ZlTnWwY4Tpc44hSXO\|YYm=	MkP2NeKh\|ryP	MlnJNE4zPS12ODDo	NEHwNYNFVVOR	MY\hZ5RqfmG2ZYOgUmYuc0J?	M1TIWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2	NX7kZnZnTnWwY4Tpc44hSXO\|YYm=	MY[xxsDPxE1?	MWmwMlI2NTR6IHi=	M1;i[mROW09?	NV7SWWll[WO2aY\heIV{KE6ILXvC	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2	NX[3V4dyTnWwY4Tpc44hSXO\|YYm=	M4rQSlAvPS9zIN88US=>	M1LzWFI1NzR6IHi=	MUXEUXNQ	NH;Q[G52eHKnZ4XsZZRmeyCWTl[t{tEh\G:\|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=>	M2HSTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428	NVjwdoJqTnWwY4Tpc44hSXO\|YYm=	MoHhNE42NzFizszN	MU[yOE81QCCq	NHLIXppFVVOR	NVrrUo1vfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk>	NFLhOXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2	NI\hUIdHfW6ldHnvckBCe3OjeR?=	NUTOfXBlOC53L{Gg{txO	MljoNlQwPDhiaB?=	NHnvPGpFVVOR	MkXueZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm=	NVzvPXFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2	Mm\3SpVv[3Srb36gRZN{[Xl?	NIrz[3QyyqEQvF2=	NXfqPIZWOjRxNEigbC=>	NY[z[HlITE2VTx?=	NEXmXXpld3ewcnXneYxifGW\|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{	NYPQNpRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428	MofnSpVv[3Srb36gRZN{[Xl?	M{i2cFHDqM7:TR?=	M3\ycVI1NzR6IHi=	M4XrfWROW09?	MU\kc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz	MnvUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2	NIqyVWpHfW6ldHnvckBCe3OjeR?=	M4r4OFHDqM7:TR?=	MVGyOE81QCCq	NGHrVmVFVVOR	M3vjZoRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM>	NFHyTWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
KM-H2	M2O0cWFxd3C2b4Ppd{BCe3OjeR?=	NF7CUmYxNjFxMD61M\|Eh\|ryP	M2TQcVQ5KGh?	MkD4SG1UVw>?	NWDJXZpKcW6mdXPld{BieG:ydH;zbZMh\G:\|ZTDk[ZBmdmSnboTsfS=>	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
L428	MX7BdI9xfG:\|aYOgRZN{[Xl?	NEPa[4ExNjFxMD61M\|Eh\|ryP	MlW3OFghcA>?	NEHpPJZFVVOR	MkfNbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2	M4LCemFxd3C2b4Ppd{BCe3OjeR?=	NWPHdZlbOC5zL{CuOU8yKM7:TR?=	MVK0PEBp	MYrEUXNQ	MkDmbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	NVn2dmpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2	MUHGeY5kfGmxbjDBd5NigQ>?	NFv4UYUxNjFvMjFOwG0>	M2XiU\|I1KGkEoB?=	NX\vVlU{TE2VTx?=	NIfyWFV{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx	M2joU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428	NXT6Wpg{TnWwY4Tpc44hSXO\|YYm=	NG\GNmoxNjFvMjFOwG0>	MV2yOEBpyqB?	MVfEUXNQ	NHKyUFV{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2	NUn6[JpiTnWwY4Tpc44hSXO\|YYm=	MUmwMlEuOiEQvF2=	MnrnNlQhcMLi	NGq4c5FFVVOR	NUDzV4t{e2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB\|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=>	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NF\wOlY4OsLiaB?=	NIXzdWxFVVOR	MXnJR\|UxRTJwOE[g{txO	NHK3UoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
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H1299	NHz6XphCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=				NWLnOFRvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{whUUN3ME2xMlQ1\|ryP	MnXuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF4NUCyNlEoRjJzNkWwNlIyRC:jPh?=
HCT116	MWjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?				MknrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKQ2SxNVYh[2WubIOsJGlEPTB;MD6zNe69VQ>?	M4jBelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{SyOFk3Lz5{MUe0NlQ6PjxxYU6=
Sf9	NIjORodHfW6ldHnvckBie3OjeR?=		MUOyJIhzew>?		MVXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEiGQVOxJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiaX7jeYJifGWmIH\vdkAzKGi{czD1d4lv\yCUSFvLMWFkKG[udX;yc4dmdmmlIIP1ZpN1emG2ZTygTWM2OD1yLkGwNu69VQ>?	MnXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMEmyNFMoRjJ\|MEC5NlA{RC:jPh?=
HCT116	MlrlR5l1d3SxeHnjbZR6KGG\|c3H5		M3OxfVczKGi{cx?=		MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlMzP87:TR?=	M3HzUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkC2PFY4Lz5{M{KwOlg3PzxxYU6=
A549	MnzjR5l1d3SxeHnjbZR6KGG\|c3H5		M17NcFczKGi{cx?=		M{X5eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlI4Qc7:TR?=	Mo[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{ME[4OlcoRjJ\|MkC2PFY4RC:jPh?=
MCF7	Mnf2R5l1d3SxeHnjbZR6KGG\|c3H5		NVjVb5YyPzJiaILz		NWDQ[\|JxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQvQDB5zszN	M3LyblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MkC2PFY4Lz5{M{KwOlg3PzxxYU6=
HCT116	NH3EXYhEgXSxdH;4bYNqfHliYYPzZZk>		M4rF[lczKGi{cx?=		MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgcYVie3W{aX7nJINmdGy3bHHyJGFVWCCuZY\lcEBi\nSncjC3NkBpenNiYomgZ4VtdC22aYTldkBodG9iYYPzZZktKEmFNUC9NE44\|ryP	M2jyWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEK5OFg{Lz5{M{iyPVQ5OzxxYU6=
MCF7	NYixWlZ[S3m2b4TvfIlkcXS7IHHzd4F6		NEnjR4k4OiCqcoO=		M4jJ[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgcYVie3W{aX7nJINmdGy3bHHyJGFVWCCuZY\lcEBi\nSncjC3NkBpenNiYomgZ4VtdC22aYTldkBodG9iYYPzZZktKEmFNUC9NU4zPs7:TR?=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh{OUS4N{c,OjN6Mkm0PFM9N2F-
A549	M2XtWGN6fG:2b4jpZ4l1gSCjc4PhfS=>		MkLnO\|IhcHK\|		NXzpNI5wS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDifUBu\WG\|dYLpcoch[2WubIXsZZIhSVSSIHzleoVtKGGodHXyJFczKGi{czDifUBk\WyuLYTpeIVzKGeubzDhd5NigSxiSVO1NF0yNjd\|zszN	NEXEelI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyPVQ5Oyd-MkO4Nlk1QDN:L3G+
DU145	MYXDfZRwfG:6aXPpeJkh[XO\|YYm=		NXrNRnIxPzJiaILz		MkXzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYomgcYVie3W{aX7nJINmdGy3bHHyJGFVWCCuZY\lcEBi\nSncjC3NkBpenNiYomgZ4VtdC22aYTldkBodG9iYYPzZZktKEmFNUC9Nk4xPs7:TR?=	NFSxXW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyPVQ5Oyd-MkO4Nlk1QDN:L3G+
Jurkat	M2nHbmFxd3C2b4Ppd{Bie3OjeR?=	M4DiN\|EhfG9iMUCgeW0>	Mk\uNlQhcHK\|		M3T2[2lv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSoXyb4F1KGOnbHzzJIF{e2W\|c3XkJIF{KFCDUmCgZ4xm[X[jZ3WgZZQhOSC2bzCxNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh{OUS4N{c,OjN6Mkm0PFM9N2F-
HeLa	NF\ieItHfW6ldHnvckBie3OjeR?=	MlLGNUB1dyBzMDD1US=>	MWmyOEBpenN?		MYnJcohq[mm2aX;uJI9nKEiGQVOgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDIN2s6SWNibHX2[Ywh[XRiMTD0c{AyOCC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	M1v2b\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEK5OFg{Lz5{M{iyPVQ5OzxxYU6=
Jurkat	Mn6wSpVv[3Srb36gZZN{[Xl?	NH7ObmMyKHSxIEGwJJVO	MX:yOEBpenN?		M1nETGlvcGmkaYTpc44hd2ZiSFTBR{BqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hUDONOVHjJIxmfmWuIHH0JFEhfG9iMUCgeW0h[W[2ZYKgNlQhcHK\|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	NUfZWWkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4Nlk1QDNpPkKzPFI6PDh\|PD;hQi=>
High5	NHrXV2pHfW6ldHnvckBie3OjeR?=		MlniN{B1dyB{NDDodpM>		M3r6dmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiSFTBR\|Eh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJIlve2WldDDobYdpPSClZXzsd{B2e2mwZzDBZ{1NgXNvVInyMWx6eyBqZYDzbYxwdi2jY3X0fYwqNUGPQzDhd{B{fWK\|dILheIUh[W[2ZYKgN{B1dyB{NDDodpMh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR\|UxRTBwOUZOwG0>	MlfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOUWwNVgoRjJ2MEm1NFE5RC:jPh?=
HCT116	MWHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M1XndFczKGi{cx?=		MlLnRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO\|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkW3{txO	NXLIb2VbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPVUxOThpPkK0NFk2ODF6PD;hQi=>
A549	M1LzfGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MVS3NkBpenN?		Mn\rRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDNUS5JINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS54Nd88US=>	M1fBXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEm1NFE5Lz5{NEC5OVAyQDxxYU6=
High5	M3W2PWZ2dmO2aX;uJIF{e2G7		M3nublMhfG9iMkSgbJJ{		NI\h[nVKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFjERWM{KGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBqdnOnY4SgbIlocDViY3XscJMhfXOrbnegRYMuVHm\|LWT5dk1NgXNiKHXwd4ltd25vYXPleJltMS2DTVOgZZMhe3Wkc4TyZZRmKGGodHXyJFMhfG9iMkSgbJJ{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OD1zLk[3{txO	NHPq[FA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC5OVAyQCd-MkSwPVUxOTh:L3G+
SNU16	NH7Pd3ZEgXSxdH;4bYNqfHliYYPzZZk>		M1;1cVczKGi{cx?=		Mn:3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25WOTZiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF2Mt88US=>	MnjhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW0OFYoRjJ3OEC1OFQ3RC:jPh?=
High5	NUTXZZFmTnWwY4Tpc44h[XO\|YYm=		NXvE[nprOjRiaILz		MXzJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEiGQVOyJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDpcpNm[3RiSHnnbFUh[2WubIOgeZNqdmdiQXOtUJl{NVS7cj3MfZMhMGWyc3nsc44u[WOndInsLU1CVUNiYYOgd5Vje3S{YYTlJIFnfGW{IEK0JIhzeyCkeTDmcJVwemW\|Y3XuZ4Uh[XO\|YYmsJGlEPTB;MD6xO:69VQ>?	NV7xb\|FtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NFU1PDZpPkK1PFA2PDR4PD;hQi=>
High5	NVnl[Fg{TnWwY4Tpc44h[XO\|YYm=		M4PZelMhcHK\|		MX3Jcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEiGQVOzJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDpcpNm[3RiSHnnbFUh[2WubIOgeZNqdmdiQXOtUJl{NVS7cj3MfZMhMGWyc3nsc44u[WOndInsLU1CVUNiYYOgd5Vje3S{YYTlJIFnfGW{IEOgbJJ{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OD1yLkO2{txO	MnvTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW0OFYoRjJ3OEC1OFQ3RC:jPh?=
High5	NHrYclBHfW6ldHnvckBie3OjeR?=		NXK1S2V[OjRiaILz		NV:yOJJZUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDISGFEOSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhcW6\|ZXP0JGhq\2h3IHPlcIx{KHW\|aX7nJGFkNUy7cz3UfZIuVHm\|IDjldJNqdG:wLXHj[ZR6dClvQV3DJIF{KHO3YoP0doF1\SCjZoTldkAzPCCqcoOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwQVAvOzoQvF2=	MojJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW0OFYoRjJ3OEC1OFQ3RC:jPh?=
HCT116	MmPLR5l1d3SxeHnjbZR6KGG\|c3H5		M3HnbVczKGi{cx?=		M4\BN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwM{m2{txO	NU[y[4VqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NFU1PDZpPkK1PFA2PDR4PD;hQi=>
SW620	MXzDfZRwfG:6aXPpeJkh[XO\|YYm=		M{nOXFczKGi{cx?=		M{\BVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyIHPlcIx{KGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC52MUpOwG0>	Mny0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW0OFYoRjJ3OEC1OFQ3RC:jPh?=
MKN45	MYDDfZRwfG:6aXPpeJkh[XO\|YYm=		MYG3NkBpenN?		NGrZNJpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOU052NTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwNkJOwG0>	NHm2TVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwOVQ1Pid-MkW4NFU1PDZ:L3G+
Hep3B	M3HLZ2N6fG:2b4jpZ4l1gSCjc4PhfS=>		NIXsWXc4OiCqcoO=		Ml;IR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxO0JiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjh{M988US=>	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThyNUS0Okc,OjV6MEW0OFY9N2F-
HepG2	NWnzU\|ZjS3m2b4TvfIlkcXS7IHHzd4F6		NXW0bVg{PzJiaILz		NGXvS21EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwOEe2{txO	NULKOVF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NFU1PDZpPkK1PFA2PDR4PD;hQi=>
SNU5	M1vGRmN6fG:2b4jpZ4l1gSCjc4PhfS=>		NWXn[YpxPzJiaILz		NVrneWxNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06XNTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTFwMEC5{txO	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThyNUS0Okc,OjV6MEW0OFY9N2F-
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SJSA1	MorBR5l1d3SxeHnjbZR6KGG\|c3H5		MlnpO\|IhcHK\|		M3;pcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNLW0FzIHPlcIx{KGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oy54MkVOwG0>	MlrBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW0OFYoRjJ3OEC1OFQ3RC:jPh?=
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BT-37	Moq5dWhVWyCjc4PhfS=>				NE\PSWNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN\|ch[2WubIO=	NY\oepF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1	NGLYcnZyUFSVIHHzd4F6				Mn7hdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ\|Eh[2WubIO=	NX;DT3o2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Saos-2	M{fTV5FJXFNiYYPzZZk>				MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy\|	M4nib\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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NB1643	NGrLOI5yUFSVIHHzd4F6				NGj2RmhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz	MnLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
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Rh18	NFS0VllyUFSVIHHzd4F6				MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>?	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
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MG 63 (6-TG R)	MW\xTHRUKGG\|c3H5				MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	NHnTfYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
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A673	NEHTSGZyUFSVIHHzd4F6				M1nkeZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq	NFHMeWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
DAOY	MmDWdWhVWyCjc4PhfS=>				MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDERW9[KGOnbHzz	M1\UZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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RD	NXLlbHlYeUiWUzDhd5NigQ>?				NXrX[IQxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWkRiY3XscJM>	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh18	NUT0WVRGeUiWUzDhd5NigQ>?				M3XjU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOThiY3XscJM>	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh30	NGXsVYtyUFSVIHHzd4F6				MkLhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog{OCClZXzsdy=>	NYi2OlhjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Sf9	Mmn3SpVv[3Srb36gZZN{[Xl?				MoLuTY5pcWKrdHnvckBCe3OjeUqgTGRCSyCrbnjpZol1cW:wIHHzd4F6eyC5ZYLlJJBmem[xcn3l[EBjgSCUZXHjeIlwdiCEaX;sc4d6KEOxcoCuJEhO[Wy4ZYLuMEBR[S5rIIXzbY5oKGm\|b3zheIVlKGi3bXHuMEBz\WOxbXLpcoFvfCCodXzsMYxmdme2aDDISGFEOSCjbnSgMVYh\nKxbTDhJIJi[3Wub4\pdpV{KGW6cILld5Nqd25ic4nzeIVuKGmwIGPmPUBk\WyuczygTWM2OD1yLkGwNu69VQ>?	Mmn1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HCT116	M4G5TGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MlfEOFghcHK\|		Mn3hRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4zPM7:TR?=	M2PzUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4Ojl6MD:nQmNpTU2ETEyvZV4>
MCF7	MVTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NI\rU5E4OiCqcoO=		M4jPNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2yMlQ6\|ryP	M1z0WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4Ojl6MD:nQmNpTU2ETEyvZV4>
HeLa	NXzSNoZ{SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NVnE[Ww6PDhiaILz		MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;Mz6zNu69VQ>?	NVXmfYx5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
HeLa	MUPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NHWzS444OiCqcoO=		NHWw[G9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9N{41Os7:TR?=	NIHTZZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK\|5EcEWPQly8M4E,
HCT116	NHLZ[3dCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		Mlr4O\|IhcHK\|		NUfzcHJ[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oy53Md88US=>	NIfB[2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK\|5EcEWPQly8M4E,
HepG2	NVrrOlRRSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3i1blQ5KGi{cx?=		NFXFUGJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQvODYQvF2=	M3;KR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4Ojl6MD:nQmNpTU2ETEyvZV4>
HepG2	NXzMcJRQSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MXW3NkBpenN?		NWrvSHRNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01NjJ3zszN	MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HepG2	MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M2jX[lI1KGi{cx?=		MmLzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME21Mlc6\|ryP	NEDBNVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK\|5EcEWPQly8M4E,
A549	MnTRRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MnTLO\|IhcHK\|		NUfQdpFsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEyNjh5zszN	NF\NZWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK\|5EcEWPQly8M4E,
A549	NWLhR4w1SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NHX6VGE1QCCqcoO=		MnPlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDNUS5JINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUG0MlU4\|ryP	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO\|I6QDBxJ{7DbGVOSkx:L3G+
HCT116	NHXzWohCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M3TFeVI1KGi{cx?=		NIHP[YhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zQS54Od88US=>	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO\|I6QDBxJ{7DbGVOSkx:L3G+
HeLa	MWnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MYmyOEBpenN?		Mn\zRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZVzhJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUSzMljPxE1?	NF[wZZk9[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 Cell Death Discov (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 PLoS One 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 EMBO Mol Med 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 Stem Cells Transl Med 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 Oncotarget 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]	- Collapse 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]	- Collapse 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]	- Collapse Animal Models: Female CD-1 nude mice bearing H1437 tumors Dosages: 80 mg/kg Administration: Administered via p.o. (Only for Reference)

References

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 Download Mocetinostat (MGCD0103) SDF

Molecular Weight	396.44
Formula	C₂₃H₂₀N₆O
CAS No.	726169-73-9
Storage	3 years-20°C powder 2 years-80°C 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

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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. )

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

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

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HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

Selective HDAC Inhibitors

Rocilinostat (ACY-1215) : HDAC5-selective, IC50=5 nM.
Most Potent HDAC Inhibitor

Quisinostat (JNJ-26481585) : HDAC1, IC50=0.11 nM; HDAC2, IC50=0.33 nM.
FDA-approved HDAC Inhibitor

Vorinostat (SAHA, MK0683) : Approved by FDA against cutaneous T cell lymphoma.
Newest HDAC Inhibitor

RG2833 (RGFP109) ^New : Brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

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Panobinostat (LBH589)

Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
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Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Entinostat (MS-275)

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Trichostatin A (TSA)

Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.
Romidepsin (FK228, Depsipeptide)

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.

Features:More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
Tubastatin A

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Mocetinostat (MGCD0103)