EM127

SKU: orb1689253

Description

EM127 is a potent, selective covalent inhibitor of SMYD3 (KD = 13 µM) that suppresses its methyltransferase activity, ERK1/2 phosphorylation, and target gene transcription. This compound is a valuable research tool for investigating SMYD3-positive cancers in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1886879-71-5
• MW: 311.76
• Purity: 97.61% (May vary between batches)
• Formula: C₁₄H₁₈ClN₃O₃
• SMILES: ClCC(=O)N1CCC(CC1)NC(=O)c1cc(on1)C1CC1
• Target: ERK|||Histone Methyltransferase
• Solubility: DMSO:20 mg/mL (64.15 mM)

Bioactivity

• In Vitro:
  In MDA-MB-231 and HCT116 cells, EM127 exhibits good anti-proliferative activity when treated with 5 μM for 24, 48, and 72 hours. Additionally, at the same concentration and time points, EM127 diminishes the expression of SMYD3 target genes. However, this effect is not observed when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells. Furthermore, in both HCT116 and MDA-MB-231 cells, EM127, at concentrations of 1, 3.5, and 5 μM for 48 and 72 hours, decreases ERK1/2 phosphorylation in a dose- and time-dependent manner.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SMYD3, ERK2, ERK1, Histone Methyltransferase, HistoneMethyltransferase

Compound Identifiers

PubChem CID

118949515