A Database of Epigenetic Modifiers
This page allow users to browse dbEM proetins by their respective names available in the table. Apart from protein names, this table comprises of five more fields. (i) Link to Uniprot (ii) Link to Deathbase (iii) Link to homologues proteins available in NCBI (iv) Link to structures available in PDB and (v) Link to BioAssays available in PubChem. Please click here for help.
| DrugBank/PubChem ID | Name of Drug | Class | Chemical Class | Target | Therapeutic Use | Clinical Trial Status | Mode of Action |
|---|---|---|---|---|---|---|---|
| DB00928 | Acitidine | DNMT inhibitor | nucleoside analog | DNMT1 | FDA approved use for treatment of myelodysplastic syndrome (MDS) | FDA approved | It incorporates into RNA and traps DNMT1 enzyme resulting in loss of DNA methylatiion in nascent strand |
| NA | MGC8 | DNMT inhibitor | Antisense oligodeoxynucleotides | DNMT1 | MGC8 in combination with interferon alpha-2beta for treatment of metatstatic renal carcinoma(RCC). Clinical trials for treatment of MDS and acute myeloid leukemia (AML) | Phase I trial for MDS and AML | It is directed to bind to 3' untranslated region of DNMT1 and induces demethylation of DNA and reexpression of hypermethylated genes as p16. |
| NA | 1-BET 151 | BET protein inhibitor | Dimethylisoxazole template | BET family proteins | Preclinical studies showed anticancer activity in multiple AML | Clinical trials for AML | NA |
| 52912222 | 1-BET 762 | BET protein inhibitor | 1,4-Benzodiazepine skeleton based | BET family proteins | Preclinical studies showed inhibition of myeloma progression. | Clinical trials for myeloma | NA |
| 73087 | 3-Deazaneplanocin | HMT inhibitor | NA | HMT (Selective inhibitor of EZH2 enzyme) | NA | NA | NA |
| 76285486 | A-366 | HMT inhibitor | NA | HMT (selective inhibitor of G9a) | NA | NA | NA |
| 167551 | Anacardic acid | HATS inhibitor (p300(KAT3B) and pCAF (KAT2B) inhibitors | natural compound | HATS (p300 , IC50 7 uM and pCAF, IC50-5uM) | NA | NA | NA |
| 25150857 | BIX-01294 | HMT inhibitor | HMT (selective inhibitor of G9a mediated H3K9me2) | selective inhibitor of G9a-mediated H3K9me2 (IC50 OF 1.7) | NA | Its inhibitory effect is due to protein protein interaction alteration by occupying histone binding pocket of HMTs rathe rthan competition with SAM | |
| 1285941 | C646 | HAT inhibitor (p300) | pyrazolone | HATS | NA | NA | It is competitive p300 inhibitor versus acetyl CoA thus it binds to p300 in the active sites thus excluding acetyl-CoA. |
| 3246390 | Cambinol | Sirtuin inhibitor (SIRT1, SIRT2 inhibitor) | Hydroxynapthaldehyde derivatives | Sirtuins | Cambinol was reported to inhibit tumor growth in Burkitts's lymphoma xenograft models by inducing apoptosis through acetylation of p53 and BCL6 | NA | The C pocket of sirtuin is the proposed binding site for cambinol |
| 161591 | Chaetocin | HMT inhibitor | epidithiodiketopiperazine (natural product) | SU (VAR)3-9 CLASS OF KMTs | In vitro studies showed anticancer activities in case of primary myeloma and human tumor cell lines. | NA | NA |
| 969516 | Curcumin | HAT inhibitor (p300) | natural compound | HATS | It used as either alone or in combination with other agents is effective against colorectal, pancreatic, breast, prostrate cancer as well as multiple myeloma and head and neck carcinoma. | 35 clinical trials at various phases are going with curcumin in form of nanoparticles, capsules and solutions. | NA |
| DB01262 | Decitabine | DNMT inhibitor | nucleoside analog | DNMT1 | FDA approved use for treatment of myelodysplastic syndrome (MDS) | FDA approved | It incorporates into DNA and traps DNMT1 enzyme resulting in loss of DNA methylatiion in nascent strand |
| 99681 | Dihydro-5-azacytidine (DHAC) | DNMT inhibitor | nucleoside analog | DNMT1 | NA | NA | NA |
| 72199293 | EI1 | HMT inhibitor | non-SAM derived catalytic inhibitors | NA | NA | NA | |
| DB03823 | Epigallocatechin-3-gallate | DNMT inhibitor | non nucleoside inhibitor | DNMT1 | It shows cytotoxic effecct in human cancer cell lines | NA | It inhibits DNMT1 activity in human cancer cell lines by binding and blocking DNMT1 |
| 57345410 | EPZ-5676 | HMT inhibitor | nucleoside analogue | HMT (DOT1L) | It inhibits DOT1L mediated H3K79 methylation and suppresses leukemogenic genes. Its in clinical trials for heamtological cancers including acute leukemia with rearrangement of MLL gene. | Phase 1 clinical trials for haematological malignancies including acute leukemia with rearrangement of MLL | NA |
| 66558664 | EPZ6438 (E7438) | HMT inhibitor | non-SAM derived catalytic inhibitors (Pyridone derivatives ) | HMT (Selective inhibitor of EZH2 enzyme) | Clinical trials for targeting EZH2 in lymphoma as well as solid tumors with increased HK27me3 levels | clinical trials targeting EZH2 in lymphoma as well as solid tumors with increased levels of H3K27me3 | NA |
| NA | Etinostat | HDAC inhibitor | benzamide derivative | HDAC 1, 2, 3, 9 (Class I and II) | Clinical trials for hematological cancers and solid tumors | Clinical trials alone or in combination with other antitumor agents for treatment of hematologoical cancers such as leukemia and melanoma as well as solid tumors including colorectal cancers | It either chelates Zn ion of catalytic site of enzyme or binds key amino acid present in the active site |
| 47751 | Fazarabine | DNMT inhibitor | nucleoside analog | NA | NA | NA | NA |
| 5281560 | Garcinol | HATS inhibitor (p300(KAT3B) and pCAF (KAT2B) inhibitors | polyisoprenylated benzophenone | HATS | It inhibits DSB repair and enhances senescence in radiosensitized A549 lung and HeLa cervical carcinoma cells. It even blocks proliferation of MCF-7 breast cancer cells in vitro. | NA | NA |
| 5275521 | GGA (Geranylgeranoic acid) | HDM inhibitor | HDM (LSD1) | In vitro studies showed anticancer properties. It leads to differentiation of neuroblastoma cells through upregulation of H3K4me2 | NA | NA | |
| 56963315 | GSK-J1 | HDM inhibitor | HDM (JmjC demthylase inhibitor) | It shows reduction in cancer cell proliferation in vitro and in human xenograft models | NA | It acts by competitively binding 2-oxogluturate repositioning the metal cofactor of the active site inhibiting demethylase reaction. | |
| DB01275 | Hydralazine | DNMT inhibitor | non nucleoside inhibitor | NA | Used in combination with standard chemotherapuetics in patients with advanced solid tumors | Phase II trials | It inhibits DNA methylationby directly binding to catalytic site of DNMT1 |
| NA | Isothiazolone | HATS inhibitor (p300(KAT3B) and pCAF (KAT2B) inhibitors | NA | HATS | Inhibits strongly cell proliferation in human colon and ovarian cancer | NA | NA |
| NA | JQ1 (thieno-triazolo-1,4-diazepine) | BET protein inhibitor | Diazepine skeleton based | BET family proteins | Anticancer activity shown in xenograft models of NUT midline carcinoma, and leukemic activity shown in vitro and in vivo studies | NA | NA |
| 45029394 | Lys-CoA | HATS inhibitor (p300(KAT3B) and pCAF (KAT2B) inhibitors | Bisubstrate analogues | HATS | NA | NA | NA |
| 9865515 | Mocetinostat | HDAC inhibitor | benzamide derivative | HDAC 1, 2 (Class I and II) | It induces apoptosis in maliganat cells and detabilises microtubule formation in mitosis enhancing its cancer cytotoxicity. It was shown to inhibit autopahgy in chronic lymphocytic leukemia (CLL) | Phase 1 and Phase2 trials for hematological malignancies and solid tumors | NA |
| DB02701 | Nicotinamide and NAD analogues | Sirtuin inhibitor | Nicotinamide | Sirtuins | Nicotinamide mediated inhibition of SIRT1 showed anticancer activity in B-cell CLL and in prostrate cancer | NA | NAD inhibits SIRT activity by binding to enzyme pocket and NAD-analogues compete with NAD+ for NAD+ binding domain inhibiting enzyme activity |
| NA | NU9056 (1,2-bis (isothiazol-5yl) disulfane) | HATS inhibitor (KAT5 (Tip60) inhibitor | NA | HATS | Inhibits cell prolifeartion and induces apoptosis via caspase 3 and caspase 9 in different prostrate cancer cell lines | NA | It inhibits cell proliferation and even induces apoptosis in cancer cell lines. |
| NA | ORY-1001 | HDM inhibitor | tranylcypromine-based inhibitor | HDM (LSD1) | It was shown to induce reduction of tumor growth in vivo and in vitro | Ready to enter in Phase1 clinical trials for MLL treatment | NA |
| 6918837 | Panobinostat | HDAC inhibitor | hydroxamic acid | HDACS (Class I and II) | Clinical trials for treatment of CTCL, non-Hodgkin's and Hodgkin's lymphoma. | Phase I trials for treatment of CTCL and refractory Hodgkin's or non-Hodgkin's lymphoma. | The hydroxamic group of molecule binds to Zn ion of cataltyic site. |
| DB05103 | Pivanex | HDAC inhibitor | short chain fatty acid analogue | HDACS (Class I and II) | Clinical trials for treatment of leukemia and lymphoma | NA | It acts by destroying the catalytic activity of HDAC enzymes by interacting with Zn+2and hydrophobic pocket of enzymes. |
| NA | Polyamine conjugates | HATS inhibitor | synthetic derivatives of acetyl CoA | HATS | NA | NA | NA |
| DB00721 | Procaine | DNMT inhibitor | non nucleoside inhibitor (derivative of 4-amino benzoic acid) | DNMT1 | Used in combination with valproic acid for treatment of advanced solid tumors | Phase I trial | It inhibits DNA methylationby directly binding to catalytic site of DNMT1 |
| 6400741 | Psammaplin A | DNMT and HDAC inhibitor | non nucleoside inhibitor | DNMTas well HDACs | It shows strong cytotoxic effect in different human tumor cells lines and A549 lung xenograft models | NA | It inhibits both DNMT1 and HDACs |
| DB02709 | Resveratrol | Sirtuin activator (SIRT1 activator) | polyphenol | Sirtuins | It shows anticancer properties by use of xenograft models | NA | It prevents cancer through the activation of SIRT1 and the consequent downregulation of proteins associated with cancer progression. |
| 702558 | RG108 | DNMT inhibitor | non nucleoside inhibitor (derivative of propionic acid) | DNMT1 | In vitro studies exhibit its anticancer activity against human prostate cancer | NA | NA |
| 5352062 | Romidepsin | HDAC inhibitor | cyclic peptide | HDAC 1, 2, 4, 6 (Class I and II) | FDA approved use for treatment of CTCL and in clinical trials for treatment of solid tumor in combination with chemotherapeutic drugs | FDA approved for treatment of CTCL | It is prodrug which gets converted in cell environment into a form which interacts with Zn ion of catalytic pocket of HDACs. |
| DB01752 | SAH (S-adenosyl-L-homocysteine) | HMT inhibitor | analogue of SAM (S-adenosyl methionine) | NA | NA | NA | |
| 5113032 | Selisistat | Sirtuin inhibitor (SIRT1, SIRT2, SIRT3 inhibitor) | Indole | Sirtuins | Combination treatment with EX-527 and HDACi was found to induce apoptosis in AML cells. | NA | NA |
| 65482 | Sinefungin | HMT inhibitor | structural analogue of SAM and SAH | HMTs | It demonstrates limited effect against HMTs. | NA | NA |
| 5222465 | Sodium butyrate | HDAC inhibitor | short chain fatty acid | HDACS (Class I and II) | Induced colon cancer growth arrest and inhibition of prostrate , endometrial and cervical carcinomas | Failed clinical trials | It acts by destroying the catalytic activity of HDAC enzymes by interacting with Zn+2and hydrophobic pocket of enzymes. |
| NA | SRT1460 | Sirtuin activator (SIRT1 activator) | NA | Sirtuins | NA | NA | It is unrelated to resveratol but activates SIRT1 1000 fold more than resveratol |
| DB04786 | Suramin | Sirtuin inhibitor (SIRT1, SIRT2 inhibitor) | Suramin | Sirtuins | Antitumor effects of suramin in combination with cytotoxic agents were observed in xenograft models of prostrate lung and breast cancer cells. | Clinical trials for treatment of various cancer types | It inhibits SIRT activity by binding to active sites of enzyme |
| DB00752 | tranylcypromine | HDM inhibitor | NA | Inhibit colony formation of human mixed lineage leukemia (MLL) AF9 cells. | Clinical trials | It inhibits LSD by forming adducts with FAD cofactor in the AOL domain | |
| 444732 | Trichostatin A | HDAC inhibitor | hydroxamic acid | HDACS (Class I and II) | Is used in combination with cisplastin to obtain strong antitumor efficacy.It induces cell cycle arrest and death by increasing p21 transcription and reducing cyclinB1, Plk1 and survivins. TSA induces upregulation of tumor suppressor miRNAs and downregulation of oncomirs reducing clonogenicity of cancer cells | NA | It inhibits HDAC by using its phenyl group to pack inhibitor at the active site pocket while hydroxamic acid interacts and chelates zinc ion. |
| 44251522 | UNC0224 | HMT inhibitor | derivatives of chaetocin | HMT(G9a and SET7 and SET9) | Inhibits G9a-like protein (GLP) with an IC50 of 15nm and high selectivity against SET7/9 and SET8 | NA | NA |
| 46224516 | UNC0638 | HMT inhibitor | derivatives of chaetocin | HMT(G9a and GLP) | Inhibits G9a-like protein with IC-50 of 15nm and GLP with IC50 19nm | NA | NA |
| NA | UNCO631 | HMT inhibitor | derivatives of chaetocin | NA | NA | NA | NA |
| DB00313 | Valproate | HDAC inhibitor | short chain fatty acid | HDACS (Class I and II) | In AML patients arrests cell proliferation, increased apoptosis and differentiation. It has been used in combination with ATRA for AML treatment | Clinical trials for treatment of leukemia | NA |
| DB02546 | Vorinostat (SAHA) | HDAC Inhibitor | hydroxamic acid | HDACS (Class I and II) | FDA approved for treatment of cutaneous T cell lymphoma. Clinical trials for treatment of hematological cancers. | FDA approved (first epi-drug) for treatment of CTCL | The hydroxamic group of molecule binds to Zn ion of cataltyic site. |
| 7302 | y-butyrolactone | HATS inhibitor (Gcn5 (KAT2A) inhibitor | NA | HATS | NA | NA | NA |
| DB03068 | Zebularine | DNMT inhibitor | nucleoside analog | DNMT1 | Preclinical studies for treament of breast cancer and heaptocellular carcinoma | NA | It incorporates into DNA and traps DNMT1 enzyme resulting in loss of DNA methylatiion in nascent strand and reactivation of silenced genes. |