Epigenetics

Based on the concept of genetics´╝îepigenetics 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 CAS MF
Entinostat Entinostat 209783-80-2 C21H20N4O3
Vorinostat Vorinostat 149647-78-9 C14H20N2O3
Sodium 4-phenylbutyrate Sodium 4-phenylbutyrate 1716-12-7 C10H11NaO2
Tacedinaline Tacedinaline 112522-64-2 C15H15N3O2
Panobinostat Panobinostat 404950-80-7 C21H23N3O2
(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 (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 1268524-70-4 C23H25ClN4O2S
6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE 49843-98-3 C13H13ClN2O
N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide N-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide 726169-73-9 C23H20N6O
SRT1720 SRT1720 1001645-58-4 C25H24ClN7OS
Belinostat (PXD101) Belinostat (PXD101) 414864-00-9 C15H14N2O4S
SIRTINOL SIRTINOL 410536-97-9 C26H22N2O2
I-BET151 (GSK1210151A) I-BET151 (GSK1210151A) 1300031-49-5 C23H21N5O3
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 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 1346574-57-9 C31H38N6O2
ACY-1215 ACY-1215 1316214-52-4 C24H27N5O3
Pracinostat Pracinostat 929016-96-6 C20H30N4O2
(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 (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 128517-07-7 C24H36N4O6S2
MC1568 MC1568 852475-26-4 C17H15FN2O3
M344 M344 251456-60-7 C16H25N3O3
6-pentadecylsalicylic acid 6-pentadecylsalicylic acid 16611-84-0 C22H36O3
1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide 1396772-26-1 C32H37N5O3
UNC 1999 UNC 1999 1431612-23-5 C33H43N7O2
UNC 0631 UNC 0631 1320288-19-4 C37H61N7O2
5-Carboxy-8-hydroxyquinoline 5-Carboxy-8-hydroxyquinoline 5852-78-8 C10H7NO3
RG108 RG108 48208-26-0 C19H14N2O4
Lomeguatrib Lomeguatrib 192441-08-0 C10H8BrN5OS
CUDC-101 CUDC-101 1012054-59-9 C24H26N4O4
CRA-02478 CRA-02478 783355-60-2 C21H23N3O5
ITF2357 ITF2357 732302-99-7 C24H30ClN3O5
3-Cyclopentene-1,2-diol, 5-(4-aMino-1H-iMidazo[4,5-c]pyridin-1-yl)-3-(hydroxyMethyl)-, (Hydrochloride) (1:1), (1S,2R,5R)- 3-Cyclopentene-1,2-diol, 5-(4-aMino-1H-iMidazo[4,5-c]pyridin-1-yl)-3-(hydroxyMethyl)-, (Hydrochloride) (1:1), (1S,2R,5R)- 120964-45-6 C12H15ClN4O3
MS436 MS436 1395084-25-9 C18H17N5O3S
2-Propenamide, N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2E)- 2-Propenamide, N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2E)- 404951-53-7 C22H25N3O3
Droxinostat Droxinostat 99873-43-5 C11H14ClNO3
PFI-1 PFI-1 1403764-72-6 C16H17N3O4S
SP2509 SP2509 1423715-09-6 C19H20ClN3O5S
Tubacin Tubacin 537049-40-4 C41H43N3O7S
4SC-201 4SC-201 864814-88-0 C16H19N3O4S
JNJ-26481585 JNJ-26481585 875320-29-9 C21H26N6O2
GSK 525762A GSK 525762A 1260907-17-2 C22H22ClN5O2
PI3K/HDAC Inhibitor PI3K/HDAC Inhibitor 1339928-25-4 C23H24N8O4S
(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 (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 1380288-87-8 C30H42N8O3
ZEBULARINE ZEBULARINE 3690-10-6 C9H12N2O5
SPLITOMICIN SPLITOMICIN 5690-03-9 C13H10O2
PCI 34051 PCI 34051 950762-95-5 C17H16N2O3
RVX-208 RVX-208 1044870-39-4 C20H22N2O5
GSK 343 GSK 343 1346704-33-3 C31H39N7O2
SCRIPTAID SCRIPTAID 287383-59-9 C18H18N2O4
tasquinimod tasquinimod 254964-60-8 C20H17F3N2O4
UNC-1215 UNC-1215 1415800-43-9 C32H43N5O2
AR-42 AR-42 935881-37-1 C18H20N2O3
Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438) 1403254-99-8 C34H44N4O4
TMP269 TMP269 1314890-29-3 C25H21F3N4O3S
EPZ004777 EPZ004777 1338466-77-5 C28H41N7O4
UNC 669 UNC 669 1314241-44-5 C15H20BrN3O
UNC0379 UNC0379 1620401-82-2 C23H35N5O2
RGFP 109 RGFP 109 1215493-56-3 C20H25N3O2
BRD4770 BRD4770 1374601-40-7 C25H23N3O3
EPZ015666 EPZ015666 1616391-65-1 C20H25N5O3
OG-L002 OG-L002 1357302-64-7 C15H15NO
OF-1 OF-1 919973-83-4 C17H18BrN3O4S
LMK-235 LMK-235 1418033-25-6 C15H22N2O4
4SC-202 (free base) 4SC-202 (free base) 910462-43-0 C23H21N5O3S
RGFP966 RGFP966 1396841-57-8 C21H19FN4O
ReModelin hydrobroMide ReModelin hydrobroMide 1622921-15-6 C15H15BrN4S
SRT2104 (GSK2245840) SRT2104 (GSK2245840) 1093403-33-8 C26H24N6O2S2
SGC0946 SGC0946 1561178-17-3 C28H40BrN7O4
Tubastatin-A Tubastatin-A 1252003-15-8 C20H21N3O2
MM-102 MM-102 1417329-24-8 C35H49F2N7O4
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide 304896-28-4 C23H13Cl2N3O2
MI-2 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor) 1271738-62-5 C18H25N5S2
CAY10603 CAY10603 1045792-66-2 C22H30N4O6
MI-3 (Menin-MLL Inhibitor) MI-3 (Menin-MLL Inhibitor) 1271738-59-0 C18H25N5S2
SGI-1027 SGI-1027 1020149-73-8 C27H23N7O
OTX015 OTX015 202590-98-5 C25H22ClN5O2S
CPI-203 CPI-203 1446144-04-2 C19H18ClN5OS
EI1 EI1 1418308-27-6 C23H26N4O2
JIB-04 JIB-04 199596-05-9 C17H13ClN4
SGC-CBP30 SGC-CBP30 1613695-14-9 C28H33ClN4O3
BroMosporine BroMosporine 1619994-69-2 C17H20N6O4S
Nexturastat A Nexturastat A 1403783-31-2 C19H23N3O3
C 646 C 646 328968-36-1 C24H19N3O6
GSK J4 HCl GSK J4 HCl 1373423-53-0 C24H27N5O2
GSK1324726A (I-BET726) GSK1324726A (I-BET726) 1300031-52-0 C25H23ClN2O3
PFI3 PFI3 1819363-80-8 C19H19N3O2
PFI-2 PFI-2 1627676-59-8 C23H25F4N3O3S
MG149 MG149 1243583-85-8 C22H28O3
CAY10683 (SantacruzaMate A) CAY10683 (SantacruzaMate A) 1477949-42-0 C15H22N2O3
ML234 ML234 1222800-79-4 C21H23N3O2
HPOB HPOB 1429651-50-2 C17H18N2O4
BRD73954 BRD73954 1440209-96-0 C16H16N2O3
BIX 01294 BIX 01294 1392399-03-9 C28H41Cl3N6O2
GSK-LSD1 2HCl GSK-LSD1 2HCl 1431368-48-7 C14H20N2
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