EM127

• Description :

  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[1].

• UNSPSC :

  12352005

• Target :

  Histone Methyltransferase

• Type :

  Reference compound

• Related Pathways :

  Epigenetics

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/em127.html

• Purity :

  99.94

• Solubility :

  DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

  O=C(C1=NOC(C2CC2)=C1)NC3CCN(C(CCl)=O)CC3

• Molecular Formula :

  C14H18ClN3O3

• Molecular Weight :

  311.76

• References & Citations :

  [1]Parenti M D, et al. Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3. European Journal of Medicinal Chemistry, 2022: 114683.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, stored under nitrogen)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  SMYD3

• CAS Number :

  [1886879-71-5]