- LLY-507
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- $37.00 / 1mg
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2024-11-13
- CAS:1793053-37-8
- Min. Order:
- Purity: 99.93%
- Supply Ability: 10g
- LLY-507
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- $1.00 / 1KG
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2019-12-24
- CAS:1793053-37-8
- Min. Order: 1KG
- Purity: Min98% HPLC
- Supply Ability: g/kg/ton
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| | LLY-507 Basic information |
| Product Name: | LLY-507 | | Synonyms: | LLY-507;5-Cyano-2'-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)propyl]-[1,1'-biphenyl]-3-carboxamide;5-cyano-2'-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl]-N-[3-(1-pyrrol;LLY-507(CHEMBL3414623);LLY-507; LLY507;LLY 507;CS-2196;5-Cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl}-N-[3-(1-pyrrolidinyl)propyl]-3-biphenylcarboximidic acid;3-Cyano-5-[2-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl]phenyl]-N-[3-(pyrrolidin-1-yl)propyl]benzamide | | CAS: | 1793053-37-8 | | MF: | C36H42N6O | | MW: | 574.76 | | EINECS: | | | Product Categories: | | | Mol File: | 1793053-37-8.mol |  |
| | LLY-507 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | ≥57.5 mg/mL in DMSO; insoluble in H2O; ≥54.7 mg/mL in EtOH | | form | solid | | color | White to off-white |
| | LLY-507 Usage And Synthesis |
| Uses | LLY-507 is a small molecule inhibitor of SMYD2 (lysine N-methyltransferase), preventing p53 lysine methylation in squamous cell carcinoma cells. Shows a >100-fold selective for SMYD2 over 27 other protein methyltransferases (and non-methyltransferase) targets. | | Biological Activity | lly-507 is a potent inhibitor of smyd2.smyd2, a lysine methyltransferase, catalyzes the monomethylation of several protein substrates including p53. smyd2 is reported to be overexpressed in a significant percentage of esophageal squamous primary carcinomas, and such overexpression related with poor patient survival. | | in vitro | lly-507 has been identified as a cell-active, potent small molecule inhibitor of smyd2. lly-507 was found to be >100-fold selective for smyd2 over a broad range of methyltransferase and non-methyltransferase targets. the crystal structure of smyd2 in complex with lly-507 showed it bound in the substrate peptide binding pocket. lly-507 was active in cells as demonstrated by the reduction of smyd2-induced monomethylation of p53 lys(370) at submicromolar concentrations. furthermore, ms-based proteomics indicated that cellular histone methylation levels were not affected by smyd2 inhibition with lly-507 significantly, and subcellular fractionation studies showed that smyd2 was primarily cytoplasmic, indicating that smyd2 targeted a small subset of histones. moreover, lly-507 was able to inhibit the proliferation of several liver, esophageal, as well as breast cancer cell lines in a dose-dependent manner [1]. | | IC 50 | < 15 nm | | references | [1] nguyen h, et al. lly-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase smyd2. j biol chem. 2015 may 29;290(22):13641-13653. |
| | LLY-507 Preparation Products And Raw materials |
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