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Trametinib

Allosteric inhibitor of MAP2K1, MAP2K2

Structure

Information

  • MAP2K1
  • MAP2K2
  • Allosteric inhibitor
  • up to 100 nM

In Vitro Validations

Uniprot ID: Q02750
Target Class: Kinase
Target SubClass: STE
Potency: IC 50
Potency Value: 0.92 nM
Potency Assay: Raf-MEK-ERK cascade kinase assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Dual specificity mitogen-activated protein kinase ...

DOI Reference: 10.3892/ijo.2011.1015

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

No inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. No relevant inhibition detected in a panel of 99 Kinases @ 10 uM.

Probe Selectivity in Cell:

Trametinib exhibited over 50-fold selectivity for cancer cells relative to normal tissues and hematopoietic cells

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