EM127 - ≥98% , CAS No.1886879-71-5

CAS: 1886879-71-5 Cat. No.: E648888 Formule: C₁₄H₁₈ClN₃O₃ Poids moléculaire: 311.76

GRADE & PURITY ≥98%

Storage

Store at 2-8°C

Shipped In

Wet ice

Vue d’ensemble

EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity ( K D =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

In Vitro

EM127 (5 μM; 24, 48, 72 h) shows good anti-proliferative activity in MDA-MB-231and HCT116 cells. EM127 (5 μM; 24, 48, 72 h) attenuates the expression of SMYD3 target genes while does not affect expression when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells. EM127 (1, 3.5, 5 μM; 48, 72 h) decreases ERK1/2 phosphorylation in a dose- and time-dependent manner in HCT116 and MDA-MB-231cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: MDA-MB-231, HCT116 cells Concentration: 5 μM Incubation Time: 24, 48, 72 h Result: Significantly retarded cell proliferation by 48 h. RT-PCRCell Line: MDA-MB-231 cells Concentration: 0.5, 3.5, 5 μM Incubation Time: 48 h Result: Significantly reduced the expression of CDK2 and C-MET, the known SMYD3 regulated genes. Attenuated the abundance of mRNAs of the extracellular matrix component fibronectin 1 (FN1) and N-cadherin (N-CAD). Western Blot AnalysisCell Line: HCT116, MDA-MB-231cells Concentration: 1, 3.5, 5 μM Incubation Time: 48, 72 h Result: Attenuated ERK1/2 phosphorylation and induced PARP processing at the same concentrations that retarded cell proliferation.

Form:Solid

IC50& Target:SMYD3

Specifications

Spécifications et pureté

≥98%

Mécanismes biochimiques et physiologiques

EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity ( K D =13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively a

Conditions de stockage de stockage

Store at 2-8°C

Expédié en

Wet ice

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Pureté

≥98%

Noms et identifiants

• Poids moléculaire: 311.76

Foire aux questions

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at 2–8 °C. Refrigerated storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships chilled on wet ice. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1886879-71-5, the molecular formula is C14H18ClN3O3, and the molecular weight is 311.76 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.