LLY-507

SKU: orb1300382

Description

LLY-507

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1793053-37-8
• MW: 574.76
• Purity: 99.58%
• Formula: C₃₆H₄₂N₆O
• SMILES: Cc1cn(CCN2CCN(CC2)c2ccccc2-c2cc(cc(c2)C(=O)NCCCN2CCCC2)C#N)c2ccccc12
• Target: Histone Methyltransferase
• Solubility: DMSO:16.67 mg/mL (29 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:3.3 mg/mL (5.74 mM);Ethanol:21 mg/mL (36.54 mM)

Bioactivity

• Target IC50:
  SMYD2:15 nM.
• In Vitro:
  LLY-507 effectively inhibits the ability of SMYD2 to methylate p53 peptide (IC50<15 nM). LLY-507 is able to potently inhibit the methylation of the H4 peptide by the SMYD2 enzyme (IC50: 31 nM). It has 100-fold selectivity for SMYD2 than 24 other protein or DNA methyltransferases including related family members SMYD3 and SUVH420H1/SUV420H2. LLY-507 inactive (>20 μM) against three cytochrome P450 enzymes, 14 nuclear hormone receptors, 35 G protein-coupled receptors, and 454 kinases. LLY-507 dose-dependently inhibits the proliferation of several liver, esophageal, and breast cancer cell lines.
• Cell Research:
  To examine the methylation status of p53 in HEK293 cells treated with LLY-507 by Western blotting, 2 × 105 cells are seeded in 6-well plates in triplicate and co-transfected with FLAG-tagged p53 and FLAG-tagged SMYD2 using Lipofectamine 2000. The day after transfection, cells are treated with 0-2.5 μM LLY-507 for 28 h, then collected, and lysed in RIPA buffer. Cell lysates are subject to 10% SDS-PAGE and transferred to a PVDF membrane.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

protein, SMYD2, epigenetics, Inhibitor, Histone Methyltransferase, HistoneMethyltransferase, inhibit, LLY507, LLY-507, LLY 507, p53, methylation, methyltransferase, cancer, breast

Compound Identifiers

PubChem CID

91623361