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 |
|---|---|---|---|---|---|---|---|
| 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. |
| 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 |
| 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 | |
| 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 |
| 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 |
| 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. |
| 45029394 | Lys-CoA | HATS inhibitor (p300(KAT3B) and pCAF (KAT2B) inhibitors | Bisubstrate analogues | HATS | NA | 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 |
| 47751 | Fazarabine | DNMT inhibitor | nucleoside analog | NA | NA | NA | NA |