EM127 | SMYD3 inhibitor | Probechem Biochemicals

Chemical Structure : EM127

CAS No.: 1886879-71-5

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EM127 (EM 127)

货号: PC-49813Not For Human Use, Lab Use Only.

EM127 is a potent, site-specific covalent, second-generation inhibitor of SMYD3 methyltransferase.

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5 mg	￥1180	In stock
10 mg	￥1880	In stock
25 mg	￥3280	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	311.77
分子式	C14H18ClN3O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(1-(2-chloroacetyl)piperidin-4-yl)-5-cyclopropylisoxazole-3-carboxamide

参考文献

1. Marco Daniele Parenti, et al. Eur J Med Chem. 2022 Dec 5;243:114683.

EM127 (EM 127)

生物&药学活性

物理化学性质&存储条件

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EM127 (EM 127)

生物&药学活性

物理化学性质&存储条件

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