Drug General Information |
Drug ID |
D00FHR
|
Former ID |
DCL001114
|
Drug Name |
MGCD-0103
|
Synonyms |
Mocetinostat; MG 0103; MG 4230; MG 4915; MG 5026; MG0103; MG4230; MG4915; MG5206; MGCD 0103; MGCD0103; MG-0103; MG-4230; MG-4915; MG-5026; Mocetinostat, MGCD0103; N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide; N-(2-Aminophenyl)-4-((4-pyridin-3-ylpyrimidin-2-ylamino)methyl)benzamide
|
Drug Type |
Small molecular drug
|
Indication |
Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48]
|
Phase 2 |
[1],
[2]
|
Therapeutic Class |
Anticancer Agents
|
Company |
MethylGene Inc
|
Structure |
|
Download
2D MOL
3D MOL
|
Formula |
C23H20N6O
|
InChI |
InChI=1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29)
|
InChIKey |
HRNLUBSXIHFDHP-UHFFFAOYSA-N
|
PubChem Compound ID |
|
PubChem Substance ID |
14830272, 24157526, 45287781, 56269575, 57373597, 75001461, 87226489, 87350368, 99436992, 103571737, 124490381, 124757017, 125163821, 125570876, 126671642, 131480763, 134964362, 135200342, 135723831, 136340181, 136367318, 136367876, 136920348, 137061752, 137276026, 142701494, 144116214, 152254622, 152258401, 152344187, 160647238, 162011468, 162037450, 162202711, 164042034, 164193968, 171578666, 172914178, 174007066, 174530499, 175608166, 177748388, 178103587, 186007035, 187071895, 188899510, 198936135, 218902997, 223387412, 223679945
|
Target and Pathway |
Target(s) |
Histone deacetylase 1 |
Target Info |
Inhibitor |
[3],
[4],
[5]
|
KEGG Pathway
|
Cell cycle
|
Notch signaling pathway
|
Thyroid hormone signaling pathway
|
Huntington's disease
|
Amphetamine addiction
|
Alcoholism
|
Epstein-Barr virus infection
|
Pathways in cancer
|
Transcriptional misregulation in cancer
|
Viral carcinogenesis
|
MicroRNAs in cancer
|
Chronic myeloid leukemia
|
NetPath Pathway
|
TCR Signaling Pathway
|
PANTHER Pathway
|
Wnt signaling pathway
|
p53 pathway
|
Pathway Interaction Database
|
Regulation of nuclear SMAD2/3 signaling
|
Notch signaling pathway
|
E2F transcription factor network
|
Presenilin action in Notch and Wnt signaling
|
Signaling events mediated by HDAC Class I
|
Regulation of Telomerase
|
Glucocorticoid receptor regulatory network
|
Sumoylation by RanBP2 regulates transcriptional repression
|
Regulation of Androgen receptor activity
|
IL3-mediated signaling events
|
Validated nuclear estrogen receptor alpha network
|
Retinoic acid receptors-mediated signaling
|
Hedgehog signaling events mediated by Gli proteins
|
Regulation of nuclear beta catenin signaling and target gene transcription
|
Validated targets of C-MYC transcriptional repression
|
Regulation of retinoblastoma protein
|
Notch-mediated HES/HEY network
|
Reactome
|
G0 and Early G1
|
p75NTR negatively regulates cell cycle via SC1
|
Formation of the beta-catenin:TCF transactivating complex
|
NOTCH1 Intracellular Domain Regulates Transcription
|
SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription
|
Constitutive Signaling by NOTCH1 PEST Domain Mutants
|
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
|
HDACs deacetylate histones
|
Deactivation of the beta-catenin transactivating complex
|
NoRC negatively regulates rRNA expression
|
RNA Polymerase I Transcription Initiation
|
Factors involved in megakaryocyte development and platelet production
|
WikiPathways
|
SIDS Susceptibility Pathways
|
Notch Signaling Pathway
|
TGF beta Signaling Pathway
|
IL-6 signaling pathway
|
Apoptosis-related network due to altered Notch3 in ovarian cancer
|
Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer
|
Notch Signaling Pathway
|
Retinoblastoma (RB) in Cancer
|
Neural Crest Differentiation
|
TWEAK Signaling Pathway
|
Integrated Breast Cancer Pathway
|
Signalling by NGF
|
RNA Polymerase I, RNA Polymerase III, and Mitochondrial Transcription
|
Mitotic G1-G1/S phases
|
Factors involved in megakaryocyte development and platelet production
|
Cell Cycle
|
Androgen receptor signaling pathway
|
References |
REF 1 | MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68. |
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REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7008). |
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REF 3 | Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84. |
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REF 4 | Histone deacetylase inhibitors in cancer therapy: latest developments, trends and medicinal chemistry perspective. Anticancer Agents Med Chem. 2007 Sep;7(5):576-92. |
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REF 5 | Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32. |