LLY-507

Catalog No.S7575 Batch:S757501

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Technical Data

Formula

C36H42N6O
Molecular Weight 574.76 CAS No. 1793053-37-8
Solubility (25°C)* In vitro DMSO 30 mg/mL (52.19 mM)
Ethanol 22 mg/mL (38.27 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.
Targets
SMYD2 [1]
In vitro LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 is able to potently inhibit the methylation of H4 peptide by SMYD2 enzyme with an IC50 of 31 nM. It has 100-fold selectivity for SMYD2 over 24 other protein or DNA methyltransferases including related family members SMYD3, SUVH420H1, and SUV420H2. LLY-507 inactives (>20 μM) against 454 kinases, 35 G protein-coupled receptors, 14 nuclear hormone receptors, and three cytochrome P450 enzymes. LLY-507 inhibits the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HEK293 cells

  • Concentrations

    0-2.5 μM

  • Incubation Time

    28 h

  • Method

    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 radioimmunoprecipitation assay (RIPA) buffer. Cell lysates are subject to 10% SDS-PAGE and transferred to a PVDF membrane.

Selleck's LLY-507 has been cited by 5 publications

BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacol Res, 2022, 177:106122] PubMed: 35149187
The histone methyltransferase SMYD2 is a novel therapeutic target for the induction of apoptosis in ovarian clear cell carcinoma cells [ Oncol Lett, 2020, 20(5):153] PubMed: 32934721
Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition. [ J Immunother Cancer, 2019, 7(1):277] PubMed: 31653272
Histone methyltransferase SMYD2 selective inhibitor LLY-507 in combination with poly ADP ribose polymerase inhibitor has therapeutic potential against high-grade serous ovarian carcinomas. [ Biochem Biophys Res Commun, 2019, 513(2):340-346] PubMed: 30955858
Strategies for improving antitumor response in prostate cancer: BET Bromodomain inhibition and A2A Adenosine Receptor inhibition as methods of targeting prostate [ JScholarship, 2019, None] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.