For research use only. Not for therapeutic Use.
UNC0638（Cat No.:I001019）is a potent and selective inhibitor of the histone methyltransferase EZH2, which is part of the Polycomb repressive complex 2 (PRC2) and plays a critical role in regulating gene expression through trimethylation of histone H3 at lysine 27 (H3K27me3). By inhibiting EZH2, UNC0638 leads to the reactivation of silenced tumor suppressor genes and can inhibit cancer cell proliferation, particularly in hematologic malignancies and solid tumors with elevated EZH2 activity. This compound has shown promise in preclinical studies, making it a valuable tool for exploring epigenetic therapies in cancer treatment.
| Catalog Number | I001019 |
| CAS Number | 1255580-76-7 |
| Synonyms | 2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine |
| Molecular Formula | C₃₀H₄₇N₅O₂ |
| Purity | ≥95% |
| Target | Histone Methyltransferase |
| Solubility | DMSO: ≥ 34 mg/mL |
| Storage | Store at -20°C |
| IC50 | <15 nM (G9a); 19±1 nM (GLP) [1] |
| IUPAC Name | 2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine |
| InChI | InChI=1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33) |
| InChIKey | QOECJCJVIMVJGX-UHFFFAOYSA-N |
| SMILES | CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OCCCN4CCCC4)C5CCCCC5 |
| Reference | 1:Reprod Domest Anim. 2014 Apr;49(2):e21-5. doi: 10.1111/rda.12277. Epub 2014 Jan 28. Effects of the histone methyltransferase inhibitor UNC0638 on histone H3K9 dimethylation of cultured ovine somatic cells and development of resulting early cloned embryos.Fu L,Yan FX,An XR,Hou J, PMID: 24467723 DOI: 10.1111/rda.12277 </br><span>Abstract:</span> Aberrant hypermethylation of histone H3 lysine 9 (H3K9) may be involved in the developmental failure of cloned embryos. UNC0638 is a type of small molecule that can specifically inhibit the enzyme activity of histone methyltransferase EHMT2 and reduce the H3K9 dimethylation (H3K9me2) levels in cells. The objective of this study was to investigate the effect of UNC0638 in regulating H3K9me2 and development of cloned embryos. Results showed that UNC0638 could efficiently reduce H3K9me2 levels of cultured sheep foetal fibroblast cells in a concentration-dependent manner. Cloned embryos were subsequently produced from UNC0638-treated donor cells with down-regulated H3K9me2, but their in vitro development was not improved when compared with the control. Our study suggested that revision of the single histone H3K9me2 modification may be not sufficient for rescuing the development of cloned embryos. However, because of its low cellular toxicity, UNC0638 may still be a potential chemical that could be used in regulating epigenetic modification of cloned embryos. © 2014 Blackwell Verlag GmbH. |
