| Name | LLY-507 |
| Description | LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 3.3 mg/mL (5.74 mM), Sonication is recommended.
DMSO : 16.67 mg/mL (29 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 21 mg/mL (36.54 mM), Sonication is recommended.
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| Keywords | SMYD2 | protein | p53 | methyltransferase | methylation | LLY-507 | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | epigenetics | cancer | breast |
| Inhibitors Related | MAK-683 hydrochloride | SNDX-5613 | Tazemetostat | Piribedil | XY1 | UNC 0631 | （Iso）-Flavokawain A | EPZ015666 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Chromatin Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-COVID-19 Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
