UNC-1999
| CAS No. | 1431612-23-5 | Cat. No. | BCP08257 |
| Name | UNC-1999 | ||
| Synonyms | UNC 1999;UNC1999; | ||
| Formula | C33H43N7O2 | M. Wt | 569.74 |
| Description | UNC1999 was the first orally bioavailable EZH2 inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM and non-competitive with the peptide substrate. This inhibitor potently reduced H3K27me3 levels in cells and selectively killed diffused large B cell lymphoma cell lines harboring the EZH2Y641N mutant. | ||
| Pathways | Epigenetics | ||
| Targets | Histone Methyltransferase Epigenetic Reader Domain | ||
Structure
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