EM127

EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours[1].

Product Specifications

CAS Number

[1886879-71-5]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/em127.html

Purity

99.94

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=NOC(C2CC2)=C1)NC3CCN(C(CCl)=O)CC3

Molecular Formula

C14H18ClN3O3

Molecular Weight

311.76

References & Citations

[1]Parenti M D, et al. Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3. European Journal of Medicinal Chemistry, 2022: 114683.