上海莼试生物技术有限公司
上海莼试生物技术有限公司
化学性质：
| 规格 | 10mM (in 1mL DMSO) 5mg 25mg |
| CAS | 1431612-23-5 |
| 别名 | N/A |
| 化学名 | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide |
| 分子式 | C33H43N7O2 |
| 分子量 | 569.74 |
| 溶解度 | ≥ 28.5mg/mL in DMSO |
| 储存条件 | Store at -20° C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述：
UNC1999 is an orally bioavailable inhibitor of EZH2 and EZH1 with IC50 values of [1].
UNC1999 binds to the EZH2 SAM binding site of EZH2 and competes with the cofactor SAM with a Ki of 4.6nM. It does not compete with the H3 peptide substrate. UNC1999 also has potency for mutant EZH2, including Y641N and Y641F mutants. Besides EZH2, UNC1999 is effective for EZH1 with IC50 value of 45nM. UNC1999 is shown to be more than 200-fold selective for EZH2 over a broad range of non-epigenetic targets, including kinases, GPCRs, transporters and ion channels [1].
EZH2 catalyzes methylation of H3K27, producing H3K27me3. H3K27me3 is a transcriptionally repressive post-translational modification. As an inhibitor of EZH2, UNC1999 reduces H3K27me3 with IC50 value of 124nM in the In-Cell Western assay. Additionally, UNC1999 can inhibit cell proliferation in a DLBCL cell line harboring the Y641N mutant with EC50 value of 633nM. Moreover, UNC1999 is reported to be orally bioavailable in mice [1].
特别提醒：
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗，食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康，请穿好实验服并佩戴一次性手套和口罩操作。
标签：UNC1999
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