U0126

U0126

Upstate (Millipore)

1 mg

Kinase Assay

Selective inhibitor of MEK-1 and MEK-2; weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Abl, Cdk2 and Cdk4.

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The protein encoded by this gene is a member of the dual specificity protein kinase family, which acts as a mitogen-activated protein (MAP) kinase kinase. MAP kinases, also known as extracellular signal-regulated kinases (ERKs), act as an integration point for multiple biochemical signals. This protein kinase lies upstream of MAP kinases and stimulates the enzymatic activity of MAP kinases upon wide variety of extra- and intracellular signals. As an essential component of MAP kinase signal transduction pathway, this kinase is involved in many cellular processes such as proliferation, differentiation, transcription regulation and development.

FUNCTION: SwissProt: Q02750 # Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates ERK1 and ERK2 MAP kinases.
SIZE: 393 amino acids; 43439 Da
SUBUNIT: Interacts with MORG1 (By similarity). Interacts with Yersinia yopJ.
PTM: Phosphorylation on Ser/Thr by MAP kinase kinase kinases (RAF or MEKK1) regulates positively the kinase activity. & Acetylation by Yersinia yopJ prevents phosphorylation and activation, thus blocking the MAPK signaling pathway.
DISEASE: SwissProt: Q02750 # Defects in MAP2K1 are a cause of cardiofaciocutaneous syndrome (CFC syndrome) [MIM:115150]; also known as cardio-facio- cutaneous syndrome. CFC syndrome is characterized by a distinctive facial appearance, heart defects and mental retardation. Heart defects include pulmonic stenosis, atrial septal defects and hypertrophic cardiomyopathy. Some affected individuals present with ectodermal abnormalities such as sparse, friable hair, hyperkeratotic skin lesions and a generalized ichthyosis-like condition. Typical facial features are similar to Noonan syndrome. They include high forehead with bitemporal constriction, hypoplastic supraorbital ridges, downslanting palpebral fissures, a depressed nasal bridge, and posteriorly angulated ears with prominent helices. The inheritance of CFC syndrome is autosomal dominant.
SIMILARITY: SwissProt: Q02750 ## Belongs to the protein kinase superfamily. STE Ser/Thr protein kinase family. MAP kinase kinase subfamily. & Contains 1 protein kinase domain.

Upstate

C₁₈H₁₆N₆S₂

• Q02750
• P36507

2 years at -20°C

MAP Kinase/Erk Kinase (MEK), alternatively known as MKK, is a true dual-specificity kinase, in that it phosphorylates the MAP kinases on both the Thr and Tyr of the activation motif TEY. In vitro , the tyrosine phosphorylation is favored, whereas in vivo both phosphorylation events appear to occur simultaneously. This suggests that an additional factor is present in cells to facilitate the reaction. MEK1 and MEK2 are activated by phosphorylation of two serine residues (Ser218/222 in MEK1 and Ser222/226 in MEK2), which are substrates for the Raf family of kinases. Mutation of the phosphorylation sites from Ser to Asp creates a protein with constitutive kinase activity, which when expressed in cells is able to cause transformation.

Kinase

• MAP2K1
• MAPKK1
• PRKMK1
• MEK1
• MKK1

Inhibitors

U0126

NM_002755.2