Histone Methyltransferase Inhibitors HDAC inhibitors Epigenetic Reader Domain inhibitors Histone Demethylase inhibitors Histone Acetyltransferase inhibitors DNA Methyltransferase Inhibitors Sirtuin Inhibitors Sirtuin activators Epigenetic Reader Domain antagonist
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Epigenetics

Histone Methyltransferase Inhibitors HDAC inhibitors Epigenetic Reader Domain inhibitors Histone Demethylase inhibitors Histone Acetyltransferase inhibitors DNA Methyltransferase Inhibitors Sirtuin Inhibitors Sirtuin activators Epigenetic Reader Domain antagonist
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Based on the concept of genetics,epigenetics is neither simply the methylation and acetyl change caused by environmental factors in vitro, nor simply regulation by genes like transcription factor and miRNA, but a 'heritable' phenotypic alteration due to Non-DNA variation. Till now, much of so-called epigenetics research has not really extricated itself from the conception of classical genetics.

(1)   Epigenetics refers to the variation of gene expression levels due to the alteration of non-gene sequence, including DNA methylation, histone modification, chromatin remodeling and non-coding RNA regulation, which affect its function and properties mainly through regulation of the process of gene transcription or translation. The expected role of such markers are as following:
a)    To predict drug response or prognose individual differences, to guide  the treatment by optimizing and selecting a suitable medicine dose and pattern for the individual patient;
b)    As a molecular target, by reversing the abnormal epigenetic modifications, to inaugurate a new way to treat cancer.

(2)  The so-called DNA methylation means the junction of a methyl group onto the 5 'carbon of Genomic CpG dinucleotide cytosine with covalent bonds. Under normal circumstances, the CpG dinucleotidesthe of human genome "junk" sequences are relatively rare and always under the state of methylation. In contrast, the CpG islands rich in CpG dinucleotides and about the size of 100-1000bp in the human genome are always unmethylated, which are associated with 56% of the encode genes in the human genome. Human genome sequence draft analysis reveals that the number of CpG islands in the human genome is about 28,890, most of chromosomes contain 5-15 CpG islands per Mb with an average number of 10.5 CpG islands per Mb, CpG islands good correspondence. There is a good correspondence between gene number and the of density CpG islands. Because of the close relationship between DNA methylation and human development as well as tumor diseases, especially the fact of transcriptional inactivation of tumor-suppressor genes on account of the methylation of CpG island, DNA methylation has become a  significant  research task in epigenetics and epigenomics.

(3)  Abnormal "epigenetic”: epigenetics believes allergic disease is the result of the interaction of genetic and environmental factors; environmental factors can cause errors in gene expression or functional abnormalities, hence result in abnormal "epigenetic”, also known as epimutation. Environmental factors includes infections, food, passive smoking and allergens, which all can affect the differentiation  of Th1 / Th2 cell by adjusting the acetylation / deacetylation and methylation / demethylation of histone on IFN-γ and IL-4 gene locus.

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Structure:
Chemical Name:
Entinostat
CAS:
209783-80-2
MF:
C21H20N4O3
Structure:
Chemical Name:
Vorinostat
CAS:
149647-78-9
MF:
C14H20N2O3
Structure:
Chemical Name:
Sodium 4-phenylbutyrate
CAS:
1716-12-7
MF:
C10H13NaO2
Structure:
Chemical Name:
Tacedinaline
CAS:
112522-64-2
MF:
C15H15N3O2
Structure:
Chemical Name:
Panobinostat
CAS:
404950-80-7
MF:
C21H23N3O2
Structure:
Chemical Name:
(S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
CAS:
1268524-70-4
MF:
C23H25ClN4O2S
Structure:
Chemical Name:
6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE
CAS:
49843-98-3
MF:
C13H13ClN2O
Structure:
Chemical Name:
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
CAS:
726169-73-9
MF:
C23H20N6O
Structure:
Chemical Name:
SRT1720
CAS:
1001645-58-4
MF:
C25H24ClN7OS
Structure:
Chemical Name:
Belinostat (PXD101)
CAS:
414864-00-9
MF:
C15H14N2O4S
Structure:
Chemical Name:
SIRTINOL
CAS:
410536-97-9
MF:
C26H22N2O2
Structure:
Chemical Name:
I-BET151 (GSK1210151A)
CAS:
1300031-49-5
MF:
C23H21N5O3
Structure:
Chemical Name:
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
CAS:
1346574-57-9
MF:
C31H38N6O2
Structure:
Chemical Name:
ACY-1215
CAS:
1316214-52-4
MF:
C24H27N5O3
Structure:
Chemical Name:
Pracinostat
CAS:
929016-96-6
MF:
C20H30N4O2
Structure:
Chemical Name:
(1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[8.7.6]tricos-11-ene-2,5,8,19,22-pentone
CAS:
128517-07-7
MF:
C24H36N4O6S2
Structure:
Chemical Name:
MC1568
CAS:
852475-26-4
MF:
C17H15FN2O3
Structure:
Chemical Name:
M344
CAS:
251456-60-7
MF:
C16H25N3O3
Structure:
Chemical Name:
6-pentadecylsalicylic acid
CAS:
16611-84-0
MF:
C22H36O3
Structure:
Chemical Name:
1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide
CAS:
1396772-26-1
MF:
C32H37N5O3
Structure:
Chemical Name:
UNC 1999
CAS:
1431612-23-5
MF:
C33H43N7O2
Structure:
Chemical Name:
UNC 0631
CAS:
1320288-19-4
MF:
C37H61N7O2
Structure:
Chemical Name:
5-Carboxy-8-hydroxyquinoline
CAS:
5852-78-8
MF:
C10H7NO3
Structure:
Chemical Name:
RG108
CAS:
48208-26-0
MF:
C19H14N2O4
Structure:
Chemical Name:
Lomeguatrib
CAS:
192441-08-0
MF:
C10H8BrN5OS
Structure:
Chemical Name:
CUDC-101
CAS:
1012054-59-9
MF:
C24H26N4O4
Structure:
Chemical Name:
CRA-02478
CAS:
783355-60-2
MF:
C21H23N3O5
Structure:
Chemical Name:
ITF2357
CAS:
732302-99-7
MF:
C24H30ClN3O5
Structure:
Chemical Name:
3-Cyclopentene-1,2-diol, 5-(4-aMino-1H-iMidazo[4,5-c]pyridin-1-yl)-3-(hydroxyMethyl)-, (Hydrochloride) (1:1), (1S,2R,5R)-
CAS:
120964-45-6
MF:
C12H15ClN4O3
Structure:
Chemical Name:
MS436
CAS:
1395084-25-9
MF:
C18H17N5O3S
Structure:
Chemical Name:
2-Propenamide, N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2E)-
CAS:
404951-53-7
MF:
C22H25N3O3
Structure:
Chemical Name:
Droxinostat
CAS:
99873-43-5
MF:
C11H14ClNO3
Structure:
Chemical Name:
PFI-1
CAS:
1403764-72-6
MF:
C16H17N3O4S
Structure:
Chemical Name:
SP2509
CAS:
1423715-09-6
MF:
C19H20ClN3O5S
Structure:
Chemical Name:
Tubacin
CAS:
537049-40-4
MF:
C41H43N3O7S
Structure:
Chemical Name:
4SC-201
CAS:
864814-88-0
MF:
C16H19N3O4S
Structure:
Chemical Name:
JNJ-26481585
CAS:
875320-29-9
MF:
C21H26N6O2
Structure:
Chemical Name:
GSK 525762A
CAS:
1260907-17-2
MF:
C22H22ClN5O2
Structure:
Chemical Name:
PI3K/HDAC Inhibitor
CAS:
1339928-25-4
MF:
C23H24N8O4S
Structure:
Chemical Name:
(2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol
CAS:
1380288-87-8
MF:
C30H42N8O3
Structure:
Chemical Name:
ZEBULARINE
CAS:
3690-10-6
MF:
C9H12N2O5
Structure:
Chemical Name:
SPLITOMICIN
CAS:
5690-03-9
MF:
C13H10O2
Structure:
Chemical Name:
PCI 34051
CAS:
950762-95-5
MF:
C17H16N2O3
Structure:
Chemical Name:
RVX-208
CAS:
1044870-39-4
MF:
C20H22N2O5
Structure:
Chemical Name:
GSK 343
CAS:
1346704-33-3
MF:
C31H39N7O2
Structure:
Chemical Name:
SCRIPTAID
CAS:
287383-59-9
MF:
C18H18N2O4
Structure:
Chemical Name:
tasquinimod
CAS:
254964-60-8
MF:
C20H17F3N2O4
Structure:
Chemical Name:
UNC-1215
CAS:
1415800-43-9
MF:
C32H43N5O2
Structure:
Chemical Name:
AR-42
CAS:
935881-37-1
MF:
C18H20N2O3
Structure:
Chemical Name:
Tazemetostat (EPZ-6438)
CAS:
1403254-99-8
MF:
C34H44N4O4
Structure:
Chemical Name:
TMP269
CAS:
1314890-29-3
MF:
C25H21F3N4O3S
Structure:
Chemical Name:
EPZ004777
CAS:
1338466-77-5
MF:
C28H41N7O4
Structure:
Chemical Name:
UNC 669
CAS:
1314241-44-5
MF:
C15H20BrN3O
Structure:
Chemical Name:
UNC0379
CAS:
1620401-82-2
MF:
C23H35N5O2
Structure:
Chemical Name:
RGFP 109
CAS:
1215493-56-3
MF:
C20H25N3O2
Structure:
Chemical Name:
BRD4770
CAS:
1374601-40-7
MF:
C25H23N3O3
Structure:
Chemical Name:
EPZ015666
CAS:
1616391-65-1
MF:
C20H25N5O3
Structure:
Chemical Name:
OG-L002
CAS:
1357302-64-7
MF:
C15H15NO
Structure:
Chemical Name:
OF-1
CAS:
919973-83-4
MF:
C17H18BrN3O4S
Structure:
Chemical Name:
LMK-235
CAS:
1418033-25-6
MF:
C15H22N2O4
Structure:
Chemical Name:
4SC-202 (free base)
CAS:
910462-43-0
MF:
C23H21N5O3S
Structure:
Chemical Name:
RGFP966
CAS:
1396841-57-8
MF:
C21H19FN4O
Structure:
Chemical Name:
ReModelin hydrobroMide
CAS:
1622921-15-6
MF:
C15H15BrN4S
Structure:
Chemical Name:
SRT2104 (GSK2245840)
CAS:
1093403-33-8
MF:
C26H24N6O2S2
Structure:
Chemical Name:
SGC0946
CAS:
1561178-17-3
MF:
C28H40BrN7O4
Structure:
Chemical Name:
Tubastatin-A
CAS:
1252003-15-8
MF:
C20H21N3O2
Structure:
Chemical Name:
MM-102
CAS:
1417329-24-8
MF:
C35H49F2N7O4
Structure:
Chemical Name:
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
CAS:
304896-28-4
MF:
C23H13Cl2N3O2
Structure:
Chemical Name:
MI-2 (Menin-MLL Inhibitor)
CAS:
1271738-62-5
MF:
C18H25N5S2
Structure:
Chemical Name:
CAY10603
CAS:
1045792-66-2
MF:
C22H30N4O6
Structure:
Chemical Name:
MI-3 (Menin-MLL Inhibitor)
CAS:
1271738-59-0
MF:
C18H25N5S2
Structure:
Chemical Name:
SGI-1027
CAS:
1020149-73-8
MF:
C27H23N7O
Structure:
Chemical Name:
OTX015
CAS:
202590-98-5
MF:
C25H22ClN5O2S
Structure:
Chemical Name:
CPI-203
CAS:
1446144-04-2
MF:
C19H18ClN5OS
Structure:
Chemical Name:
EI1
CAS:
1418308-27-6
MF:
C23H26N4O2
Structure:
Chemical Name:
JIB-04
CAS:
199596-05-9
MF:
C17H13ClN4
Structure:
Chemical Name:
SGC-CBP30
CAS:
1613695-14-9
MF:
C28H33ClN4O3
Structure:
Chemical Name:
BroMosporine
CAS:
1619994-69-2
MF:
C17H20N6O4S
Structure:
Chemical Name:
Nexturastat A
CAS:
1403783-31-2
MF:
C19H23N3O3
Structure:
Chemical Name:
C 646
CAS:
328968-36-1
MF:
C24H19N3O6
Structure:
Chemical Name:
GSK J4 HCl
CAS:
1373423-53-0
MF:
C24H27N5O2
Structure:
Chemical Name:
GSK1324726A (I-BET726)
CAS:
1300031-52-0
MF:
C25H23ClN2O3
Structure:
Chemical Name:
PFI3
CAS:
1819363-80-8
MF:
C19H19N3O2
Structure:
Chemical Name:
PFI-2
CAS:
1627676-59-8
MF:
C23H25F4N3O3S
Structure:
Chemical Name:
MG149
CAS:
1243583-85-8
MF:
C22H28O3
Structure:
Chemical Name:
CAY10683 (SantacruzaMate A)
CAS:
1477949-42-0
MF:
C15H22N2O3
Structure:
Chemical Name:
ML234
CAS:
1222800-79-4
MF:
C21H23N3O2
Structure:
Chemical Name:
HPOB
CAS:
1429651-50-2
MF:
C17H18N2O4
Structure:
Chemical Name:
BRD73954
CAS:
1440209-96-0
MF:
C16H16N2O3
Structure:
Chemical Name:
BIX 01294
CAS:
1392399-03-9
MF:
C28H41Cl3N6O2
Structure:
Chemical Name:
GSK-LSD1
CAS:
1431368-48-7
MF:
C14H20N2