145 products were found matching "K04369"!

The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors. PD 0325901 is a potent MEK inhibitor that suppresses phosphorylation of ERK in mouse colon 26 tumors with an IC50 value of 0.33 nM. Suppression of ERK activation...

Protein function: Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases (By similarity). Activates BRAF in a KSR1 or KSR2-dependent manner, by binding to KSR1 or KSR2 releases the inhibitory...

MEK1 and MEK2, also called MAPK or Erk kinases, are dual-specificity protein kinases that function in a mitogen activated protein kinase cascade controlling cell growth and differentiation. Protein Function: Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence...

GSK1120212 inhibits MEK1/2 and is currently in clinical trials as a potential treatment for melanoma. GSK1120212 exhibits anticancer chemotherapeutic activity, upregulating p27 expression and inhibiting growth in colorectal cancer cells and suppressing tumor growth in colorectal cancer xenografts.

The protein encoded by this gene is a dual specificity protein kinase that belongs to the MAP kinase kinase family. This kinase is known to play a critical role in mitogen growth factor signal transduction. It phosphorylates and thus activates MAPK1/ERK2 and MAPK2/ERK3. The activation of this kinase itself is...

ATP + a protein = ADP + a phosphoprotein.,disease: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...

Trametinib is an inhibitor of MEK1 and -2. It inhibits B-RAF- and C-RAF-induced phosphorylation of MEK1 (IC50s = 3. and 1. nM, respectively) and MEK2 (IC50s = 1. and 0. nM, respectively). Trametinib inhibits the growth of two human colorectal cancer cell lines expressing mutant B-RAF (IC50s = 0. and 0. nM) and seven...

U-0126 is a MEK inhibitor with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively. It is noncompetitive with respect adenosine triphosphate (ATP) and its phosphorylation target ERK and it shows little to no inhibition against a number of other kinases including PKC, Ab1, Raf, MEKK, ERK, JNK, MKK-3,...

Selumetinib is a selective inhibitor of MEK1/2. Selumetinib treatment induced G1 cell-cycle arrest and apoptosis and suppression of tumor growth as xenografts in immunodeficient mice.

AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC50 = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells. AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.Formal Name:...

MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation. AZD 6244 is a potent, highly selective inhibitor of...

Trametinib is an inhibitor of MEK1 and -2. It inhibits B-RAF- and C-RAF-induced phosphorylation of MEK1 (IC50s = 3.4 and 1.8 nM, respectively) and MEK2 (IC50s = 1.6 and 0.92 nM, respectively). Trametinib inhibits the growth of two human colorectal cancer cell lines expressing mutant B-RAF (IC50s = 0.48 and 0.52 nM)...