Drug Information

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 [529426], [542038]
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
9865515
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 [536272], [536509], [537647]
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 529426MGCD0103, 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.
Ref 542038(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).
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 536509Histone deacetylase inhibitors in cancer therapy: latest developments, trends and medicinal chemistry perspective. Anticancer Agents Med Chem. 2007 Sep;7(5):576-92.
Ref 537647Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32.

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