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LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $37 | In Stock | |
2 mg | $50 | In Stock | |
5 mg | $77 | In Stock | |
10 mg | $140 | In Stock | |
25 mg | $321 | In Stock | |
50 mg | $581 | In Stock | |
100 mg | $829 | In Stock | |
1 mL x 10 mM (in DMSO) | $112 | In Stock |
Description | LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2. |
Targets&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. |
Alias | LLY507, LLY 507 |
Molecular Weight | 574.76 |
Formula | C36H42N6O |
Cas No. | 1793053-37-8 |
Smiles | Cc1cn(CCN2CCN(CC2)c2ccccc2-c2cc(cc(c2)C(=O)NCCCN2CCCC2)C#N)c2ccccc12 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 93 mg/mL (161.8 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 21 mg/mL (36.5 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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