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。

EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity ( K D =13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours [1].

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.

1886879-71-5

C14H18ClN3O3

311.76

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years