EM127 (化合物 11c) 是一种具有高选择性、高亲和力和位点特异性的SMYD3共价抑制剂 (KD=13 μM)。EM127 能有效地抑制ERK1/2磷酸化，降低SMYD3靶基因的转录调节。EM127 能够有效地和长时间地削弱甲基转移酶的活性。EM127 可用于癌症，尤其是SMYD3阳性肿瘤的研究。
| 生物活性 | EM127 (compound 11c) is aSMYD3covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibitsERK1/2phosphorylation and reduces transcriptional regulation ofSMYD3target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used incancerresearch, particularly inSMYD3positive tumours[1]. |
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体外研究
(In Vitro) | EM127 (5 μM; 24, 48, 72 h) shows good anti-proliferative activity in MDA-MB-231and HCT116 cells[1].
EM127 (5 μM; 24, 48, 72 h) attenuates the expression of SMYD3 target genes while does not affect expression when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells[1].
EM127 (1, 3.5, 5 μM; 48, 72 h) decreases ERK1/2 phosphorylation in a dose- and time-dependent manner in HCT116 and MDA-MB-231cells[1].
Cell Proliferation Assay[1] | Cell Line: | MDA-MB-231, HCT116 cells | | Concentration: | 5 μM | | Incubation Time: | 24, 48, 72 h | | Result: | Significantly retarded cell proliferation by 48 h. |
RT-PCR[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 0.5, 3.5, 5 μM | | Incubation Time: | 48 h | | Result: | Significantly reduced the expression of CDK2 and C-MET, the known SMYD3 regulated genes.
Attenuated the abundance of mRNAs of the extracellular matrix component fibronectin 1 (FN1) and N-cadherin (N-CAD). |
Western Blot Analysis[1] | Cell Line: | HCT116, MDA-MB-231cells | | Concentration: | 1, 3.5, 5 μM | | Incubation Time: | 48, 72 h | | Result: | Attenuated ERK1/2 phosphorylation and induced PARP processing at the same concentrations that retarded cell proliferation. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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