EM127

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 (KD=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.

EM127 (5 μM; 24, 48, 72 h) shows good anti-proliferative activity in MDA-MB-231and HCT116 cells.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.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-231 cells.Cell Proliferation Assay 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 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 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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Others

Other Targets

Histone Methyltransferase | ERK

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1886879-71-5

311.76

C14H18ClN3O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (80.19 mM; 超声助溶 (<60°C)

ClCC(=O)N1CCC(CC1)NC(=O)c1cc(on1)C1CC1

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(-20℃)

With Ice Pack

≥ 2 years