DEL 22379

Pricing Availability Delivery Time Qty
Cat.No. 5774 - DEL 22379 | C26H28N4O3 | CAS No. 181223-80-3
Description: ERK dimerization inhibitor
Chemical Name: N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

ERK dimerization inhibitor (IC50 ~ 0.5 μM); inhibits ERK dimerization without affecting phosphorylation or kinase activity. Suppresses growth of tumor cells expressing RAS-ERK oncogenes in vitro. Induces apoptosis and prevents tumor progression in vivo.

Technical Data

M. Wt 444.53
Formula C26H28N4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 181223-80-3
PubChem ID 11224574
InChI Key INQUULPXCZAKMS-XKZIYDEJSA-N
Smiles O=C1NC2=CC=C(NC(CCN3CCCCC3)=O)C=C2/C1=C/C4=CNC5=C4C=C(OC)C=C5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 22.23 50

Preparing Stock Solutions

The following data is based on the product molecular weight 444.53. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.25 mL 11.25 mL 22.5 mL
5 mM 0.45 mL 2.25 mL 4.5 mL
10 mM 0.22 mL 1.12 mL 2.25 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Herrero et al (2015) Small molecule inhibition of ERK dimerization prevents tumorigenesis by RAS-ERK pathway oncogenes. Cancer Cell 28 170 PMID: 26267534

Ryan et al (2015) Targeting RAS-mutant cancers: is ERK the key? Trends Cancer 1 183 PMID: 26858988


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View Related Products by Target

Keywords: ERK dimerization inhibitors inhibits extracellular signal related kinase RAS ERK

Citations for DEL 22379

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
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Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

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  • Immune Cell Signaling
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
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Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

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MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for DEL 22379

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

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