Epigenetics Pathway Inhibitors

Epigenetics defines cellular modifications that can be heritable, but appear unrelated to DNA nucleotide sequence changes, and can be modified by environmental stimuli. Epigenetic modifications include acetylation, methylation, phosphorylation, and ubiquitination and lead to changes in chromatin structure, which alter the accessibility of DNA to transcription machinery and therefore influence gene expression. During tumor development, epigenetic changes including aberrant DNA methylation and histone modification in chromatin occur frequently. These epigenetic changes are potential targets for therapeutic intervention using inhibitors of DNA methylation and histone deacetylation.

Epigenetics describes heritable changes in a cellular phenotype that are independent of alterations in the DNA sequence. Epigenetic mechanisms typically comprise DNA methylation and histone modifications, but also include many other mechanisms such as ATP-based chromatin-remodeling complexes and non-coding RNA mediated gene-silencing, as well as other mechanisms involved in generating and maintaining heritable chromatin structure. There are at least four different DNA modifications and 16 classes of histone modifications including acetylation, methylation, phosphorylation, and ubiquitination, which can alter chromatin structure by altering noncovalent interactions within and between nucleosomes. Epigenetic modifications play a critical role in the regulation of all DNA-based processes, such as transcription, DNA repair, and replication. Central to epigenetic regulation is the modulation of chromatin structure, whereby the majority of epigenetic processes impact upon chromatin organization and maintenance.

Epigenetic changes occur frequently and play an important role in tumorigenesis many HDAC inhibitors have been shown to have potent anti-tumor effects and entered clinical trials. Ongoing research is revealing the extent of the influence of epigenetics in disease states, and continues to provide a wealth of novel therapeutic targets.

Cat. No.DescriptionProduct groups

Aurora kinase antagonists

S7588Reversine [CAS no: 656820-32-5]Chemicals

Aurora kinase inhibitors

S1133Alisertib (MLN8237) (CAS no: 1028486-01-2)Chemicals
S2719AMG-900 (CAS no: 945595-80-2)Chemicals
S1134AT9283 (CAS no: 896466-04-9)Chemicals
S1451Aurora A Inhibitor I (CAS no: 1158838-45-9)Chemicals
S1147Barasertib (AZD1152-HQPA) (CAS no: 722544-51-6)Chemicals
S7843BI-847325 [CAS no: 1207293-36-4]Chemicals
S1519CCT129202 (CAS no: 942947-93-5)Chemicals
S2744CCT137690 (CAS no: 1095382-05-0)Chemicals
S1171CYC116 (CAS no: 693228-63-6)Chemicals
S1107Danusertib (PHA-739358) (CAS no: 827318-97-8)Chemicals
S1181ENMD-2076 (CAS no: 934353-76-1)Chemicals
S2018ENMD-2076 L-(+)-Tartaric acid (CAS no: 1291074-87-7)Chemicals
S2740GSK1070916 (CAS no: 942918-07-2)Chemicals
S1529Hesperadin (CAS no: 422513-13-1)Chemicals
S1249JNJ-7706621 (CAS no: 443797-96-4)Chemicals
S2158KW-2449 (CAS no: 1000669-72-6)Chemicals
S2770MK-5108 (VX-689) (CAS no: 1010085-13-8)Chemicals
S7065MK-8745 (CAS no: 885325-71-3)Chemicals
S1100MLN8054 (CAS no: 869363-13-3)Chemicals
S2725PF-03814735 (CAS no: 942487-16-3)Chemicals
S1454PHA-680632 (CAS no: 398493-79-3)Chemicals
S1154SNS-314 Mesylate (CAS no: 1146618-41-8)Chemicals
S2718TAK-901 (CAS no: 934541-31-8)Chemicals
S1048VX-680 (Tozasertib, MK-0457) (CAS no: 639089-54-6)Chemicals
S1103ZM 447439 (CAS no: 331771-20-1)Chemicals

DNA methyltransferase inhibitors

S1782Azacitidine (CAS no: 320-67-2)Chemicals
S1200Decitabine (CAS no: 2353-33-5)Chemicals
S8056Lomeguatrib (CAS no: 192441-08-0)Chemicals
S4294Procainamide HCl [CAS no: 614-39-1]Chemicals
S2821RG108 (CAS no: 48208-26-0)Chemicals
S7276SGI-1027 (CAS no: 1020149-73-8)Chemicals
S1774Thioguanine (CAS no: 154-42-7)Chemicals
S7113Zebularine (CAS no: 3690-10-6)Chemicals

Epigenetic reader domain antagonists

S7088UNC1215 (CAS no: 1415800-43-9)Chemicals

Epigenetic reader domain inhibitors

S7110(+)-JQ1 (CAS no: 1268524-70-4)Chemicals
S7304CPI-203 [CAS no: 1446144-04-2]Chemicals
S7620GSK1324726A (I-BET726) [CAS no: 1300031-52-0]Chemicals
S7231GSK2801 [CAS no: 1619994-68-1]Chemicals
S2780I-BET151 (GSK1210151A) (CAS no: 1300031-49-5)Chemicals
S7189I-BET-762 (CAS no: 1260907-17-2)Chemicals
S7305MS436 [CAS no: 1395084-25-9]Chemicals
S7681OF-1 [CAS no: 919973-83-4]Chemicals
S7360OTX015 [CAS no: 202590-98-5]Chemicals
S1216PFI-1 (PF-6405761) (CAS no: 1403764-72-6)Chemicals
S7906PFI-4 [CAS no: 900305-37-5]Chemicals
S7295RVX-208 (CAS no: 1044870-39-4)Chemicals
S7373UNC669 (CAS no: 1314241-44-5)Chemicals

HDAC inhibitors

S2341(-)-Parthenolide (CAS no: 20554-84-1)Chemicals
S75554SC-202 [CAS no: 910462-43-0]Chemicals
S2244AR-42 (CAS no: 935881-37-1)Chemicals
S1085Belinostat (PXD101) (CAS no: 414864-00-9)Chemicals
S7689BG45 [CAS no: 926259-99-6]Chemicals
S7726BRD73954 [CAS no: 1440209-96-0]Chemicals
S7596CAY10603 [CAS no: 1045792-66-2]Chemicals
S2818CI994 (Tacedinaline) (CAS no: 112522-64-2)Chemicals
S1194CUDC-101 (CAS no: 1012054-59-9)Chemicals
S2759CUDC-907 (CAS no: 1339928-25-4)Chemicals
S1703Divalproex Sodium (CAS no: 76584-70-8)Chemicals
S1422Droxinostat (CAS no: 99873-43-5)Chemicals
S1053Entinostat (MS-275) (CAS no: 209783-80-2)Chemicals
S2170Givinostat (ITF2357) (CAS no: 732302-99-7)Chemicals
S7278HPOB [CAS no: 1429651-50-2]Chemicals
S1095LAQ824 (Dacinostat) (CAS no: 404951-53-7)Chemicals
S7569LMK-235 [CAS no: 1418033-25-6]Chemicals
S2779M344 (CAS no: 251456-60-7)Chemicals
S1484MC1568 (CAS no: 852475-26-4)Chemicals
S1122Mocetinostat (MGCD0103) (CAS no: 726169-73-9)Chemicals
S7473Nexturastat A [CAS no: 1403783-31-2]Chemicals
S1030Panobinostat (LBH589) (CAS no: 404950-80-7)Chemicals
S1090PCI-24781 (Abexinostat) (CAS no: 783355-60-2)Chemicals
S2012PCI-34051 (CAS no: 950762-95-5)Chemicals
S1515Pracinostat (SB939) (CAS no: 929016-96-6)Chemicals
S1096Quisinostat (JNJ-26481585) (CAS no: 875320-29-9)Chemicals
S7292RG2833 (RGFP109) (CAS no: 1215493-56-3)Chemicals
S7229RGFP966 (CAS no: 1396841-57-8)Chemicals
S8001Rocilinostat (ACY-1215) (CAS no: 1316214-52-4)Chemicals
S3020Romidepsin (FK228, Depsipeptide) (CAS no: 128517-07-7)Chemicals
S7595Santacruzamate A (CAY10683) [CAS no: 1477949-42-0]Chemicals
S8043Scriptaid (CAS no: 287383-59-9)Chemicals
S4125Sodium Phenylbutyrate (CAS no: 1716-12-7)Chemicals
S7617Tasquinimod [CAS no: 254964-60-8]Chemicals
S7324TMP269 [CAS no: 1314890-29-3]Chemicals
S1045Trichostatin A (TSA) (CAS no: 58880-19-6)Chemicals
S2239Tubacin (CAS no: 537049-40-4)Chemicals
S8049Tubastatin A (CAS no: 1252003-15-8)Chemicals
S2627Tubastatin A HCl (CAS no: 1310693-92-5)Chemicals
S1168Valproic acid sodium salt (Sodium valproate) (CAS no: 1069-66-5)Chemicals
S1047Vorinostat (SAHA, MK0683) (CAS no: 149647-78-9)Chemicals

HIF inhibitors

S12332-Methoxyestradiol (2-MeOE2) (CAS no: 362-07-2)Chemicals
S7309BAY 87-2243 [CAS no: 1227158-85-1]Chemicals
S7979FG-2216 [CAS no: 223387-75-5]Chemicals
S1007FG-4592 (CAS no: 808118-40-3)Chemicals
S2919IOX2 (CAS no: 931398-72-0)Chemicals
S7946KC7F2 [CAS no: 927822-86-4]Chemicals
S7612PX-478 2HCl [CAS no: 685898-44-6]Chemicals

Histone acetyltransferase inhibitors

S7582Anacardic Acid [CAS no: 16611-84-0]Chemicals
S7152C646 (CAS no: 328968-36-1)Chemicals
S7476MG149 [CAS no: 1243583-85-8]Chemicals
S7641Remodelin [CAS no: 1622921-15-6]Chemicals

Histone demethylase inhibitors

S7581GSK J1 [CAS no: 1373422-53-7]Chemicals
S7070GSK J4 HCl (CAS no: 1373423-53-0)Chemicals
S7574GSK-LSD1 2HCl [CAS no: 1431368-48-7]Chemicals
S7234IOX1 [CAS no: 5852-78-8]Chemicals
S7281JIB-04 (CAS no: 199596-05-9)Chemicals
S7296ML324 [CAS no: 1222800-79-4]Chemicals
S7237OG-L002 (CAS no: 1357302-64-7)Chemicals
S7795ORY-1001 (RG-6016) [CAS no: 1431326-61-2]Chemicals
S7680SP2509 [CAS no: 1423715-09-6]Chemicals

Histone methyltransferase inhibitors

S71203-Deazaneplanocin A (DZNeP) (CAS no: 102052-95-9)Chemicals
S7884AMI-1 [CAS no: 20324-87-2]Chemicals
S8006BIX 01294 (CAS no: 1392399-03-9)Chemicals
S7591BRD4770 [CAS no: 1374601-40-7]Chemicals
S7616CPI-169 [CAS no: 1450655-76-1]Chemicals
S7656CPI-360 [CAS no: 1802175-06-9]Chemicals
S7611EI1 [CAS no: 1418308-27-6]Chemicals
S3147Entacapone (CAS no: 130929-57-6)Chemicals
S7353EPZ004777 (CAS no: 1338466-77-5)Chemicals
S7004EPZ005687 (CAS no: 1396772-26-1)Chemicals
S7748EPZ015666 [CAS no: 1616391-65-1]Chemicals
S7062EPZ5676 (CAS no: 1380288-87-8)Chemicals
S7128EPZ-6438 (CAS no: 1403254-99-8)Chemicals
S7061GSK126 [CAS no: 1346574-57-9]Chemicals
S7164GSK343 (CAS no: 1346704-33-3)Chemicals
S7804GSK503 [CAS no: 1346572-63-1]Chemicals
S7618MI-2 (Menin-MLL Inhibitor) [CAS no: 1271738-62-5]Chemicals
S7619MI-3 (Menin-MLL Inhibitor) [CAS no: 1271738-59-0]Chemicals
S7265MM-102 (CAS no: 1417329-24-8)Chemicals
S7294PFI-2 [CAS no: 1627676-59-8]Chemicals
S7079SGC 0946Chemicals
S7832SGC707 [CAS no: 1687736-54-4]Chemicals
S7610UNC0631 [CAS no: 1320288-19-4]Chemicals
S8071UNC0638 (CAS no: 1255580-76-7)Chemicals
S7165UNC1999 (CAS no: 1431612-23-5)Chemicals

JAK inhibitors

S1143AG-490 (Tyrphostin B42) (CAS no: 133550-30-8)Chemicals
S1134AT9283 (CAS no: 896466-04-9)Chemicals
S2214AZ 960 (CAS no: 905586-69-8)Chemicals
S2162AZD1480 (CAS no: 935666-88-9)Chemicals
S2851Baricitinib (LY3009104, INCB028050) (CAS no: 1187594-09-7)Chemicals
S7144BMS-911543 (CAS no: 1271022-90-2)Chemicals
S2806CEP-33779 (CAS no: 1257704-57-6)Chemicals
S7634Cerdulatinib (PRT062070, PRT2070) [CAS no: 1369761-01-2]Chemicals
S2407Curcumol (CAS no: 4871-97-0)Chemicals
S2219CYT387 (CAS no: 1056634-68-4)Chemicals
S7541Decernotinib (VX-509) [CAS no: 944842-54-0]Chemicals
S7605Filgotinib (GLPG0634)(CAS no: 1206161-97-8)Chemicals
S7259FLLL32 [CAS no: 1226895-15-3]Chemicals
S7119Go6976 [CAS no: 136194-77-9]Chemicals
S2179LY2784544 (CAS no: 1229236-86-5)Chemicals
S2686NVP-BSK805 2HCl (CAS no: 1092499-93-8)Chemicals
S8057Pacritinib (SB1518) (CAS no: 937272-79-2)Chemicals
S7650Peficitinb (ASP015K, JNJ-54781532) [CAS no: 944118-01-8]Chemicals
S1378Ruxolitinib (INCB018424) (CAS no: 941678-49-5)Chemicals
S2902S-Ruxolitinib (INCB018424) (CAS no: 941685-37-6)Chemicals
S2692TG101209 (CAS no: 936091-14-4)Chemicals
S2736TG101348 (SAR302503) (CAS no: 936091-26-8)Chemicals
S5001Tofacitinib (CP-690550) Citrate (CAS no: 540737-29-9)Chemicals
S2789Tofacitinib (CP-690550,Tasocitinib) (CAS no: 477600-75-2)Chemicals
S2867WHI-P154 (CAS no: 211555-04-3)Chemicals
S2796WP1066 (CAS no: 857064-38-1)Chemicals
S7036XL019 (CAS no: 945755-56-6)Chemicals
S8004ZM 39923 HCl (CAS no: 1021868-92-7)Chemicals

PARP inhibitors

S2197A-966492 (CAS no: 934162-61-5)Chemicals
S2178AG-14361 (CAS no: 328543-09-5)Chemicals
S7029AZD2461 (CAS no: 1174043-16-3)Chemicals
S7048BMN 673 (CAS no: 1207456-01-6)Chemicals
S7239G007-LK [CAS no: 1380672-07-0]Chemicals
S1087Iniparib (BSI-201) (CAS no: 160003-66-7)Chemicals
S1132INO-1001 (CAS no: 3544-24-9)Chemicals
S7438ME0328 (CAS no: 1445251-22-8)Chemicals
S2741MK-4827 (Niraparib) (CAS no: 1038915-60-4)Chemicals
S7730NU1025 [CAS no: 90417-38-2]Chemicals
S1060Olaparib (AZD2281, Ku-0059436) (CAS no: 763113-22-0)Chemicals
S2886PJ34 (CAS no: 344458-19-1)Chemicals
S7300PJ34 HCl (CAS no: 344458-15-7)Chemicals
S1098Rucaparib (AG-014699,PF-01367338) (CAS no: 459868-92-9)Chemicals
S8038UPF 1069 (CAS no: 1048371-03-4)Chemicals
S1004Veliparib (ABT-888) (CAS no: 912444-00-9)Chemicals

Pim inhibitors

S7104AZD1208 [CAS no: 1204144-28-4]Chemicals
S7041CX-6258 HCl [CAS no: 1353859-00-3]Chemicals
S2198SGI-1776 free base (CAS no: 1025065-69-3)Chemicals
S8005SMI-4a (CAS no: 438190-29-5)Chemicals

Sirtuin activators

S2298Fisetin (CAS no: 528-48-3)Chemicals
S2391Quercetin (CAS no: 117-39-5)Chemicals
S1396Resveratrol (CAS no: 501-36-0)Chemicals
S1129SRT1720 (CAS no: 1001645-58-4)Chemicals
S7792SRT2104 (GSK2245840) [CAS no: 1093403-33-8]Chemicals

Sirtuin inhibitors

S7577AGK2 [CAS no: 304896-28-4]Chemicals
S1541EX 527 (Selisistat) (CAS no: 49843-98-3)Chemicals
S1899Nicotinamide (Vitamin B3) (CAS no: 98-92-0)Chemicals
S7845SirReal2 [CAS no: 709002-46-0]Chemicals
S2804Sirtinol (CAS no: 410536-97-9)Chemicals
S7593Splitomicin [CAS no: 5690-03-9]Chemicals
S4900Tenovin-6 (CAS no: 1011557-82-6)Chemicals

Related to:
Brands: Selleck Chemicals
Product groups: Chemicals​