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Chemical Structure : EM127
CAS No.: 1886879-71-5
Catalog No.: PC-49813Not For Human Use, Lab Use Only.
EM127 is a potent, site-specific covalent, second-generation inhibitor of SMYD3 methyltransferase.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
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EM127 is a potent, site-specific covalent, second-generation inhibitor of SMYD3 methyltransferase.
EM127 shows a striking selectivity towards the target Cys186 residue.
EM127 is more potent than the reference inhibitor EPZ031686.
EM127 attenuated the proliferation of MDA-MB-231 breast cancer cell line at the same low micromolar range of concentrations that reduced SMYD3 mediated ERK signaling in HCT116 colorectal cancer and MDA-MB-231 breast cancer cells.
EM127 (5 μM) strongly decreased the steady-state mRNA levels of genes important for tumor biology such as cyclin dependent kinase 2, c-MET, N-cadherin and fibronectin 1, all known to be regulated, at least in part, by SMYD3.
| M.Wt | 311.77 | |
| Formula | C14H18ClN3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
N-(1-(2-chloroacetyl)piperidin-4-yl)-5-cyclopropylisoxazole-3-carboxamide |
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1. Marco Daniele Parenti, et al. Eur J Med Chem. 2022 Dec 5;243:114683.
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