Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 37.00 | |
2 mg | In stock | $ 50.00 | |
5 mg | In stock | $ 77.00 | |
10 mg | In stock | $ 140.00 | |
25 mg | In stock | $ 321.00 | |
50 mg | In stock | $ 581.00 | |
100 mg | In stock | $ 829.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 112.00 |
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. |
Synonyms | LLY507, LLY 507 |
Molecular Weight | 574.76 |
Formula | C36H42N6O |
CAS No. | 1793053-37-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (161.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 21 mg/mL (36.5 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
LLY-507 1793053-37-8 Chromatin/Epigenetic Histone Methyltransferase protein LLY507 inhibit methyltransferase methylation breast cancer LLY 507 SMYD2 p53 Inhibitor epigenetics inhibitor