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Technical Data
| Formula | C36H42N6O |
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| Molecular Weight | 574.76 | CAS No. | 1793053-37-8 | |
| Solubility (25°C)* | In vitro | DMSO | 16 mg/mL (27.83 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. | |
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| 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)
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Selleck's LLY-507 has been cited by 6 publications
| The lysine methyltransferase SMYD2 facilitates neointimal hyperplasia by regulating the HDAC3-SRF axis [ Acta Pharm Sin B, 2024, 14(2):712-728] | PubMed: 38322347 |
| 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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.