FR 180204

• Supplier: Tocris Bioscience
• Catalog: 3643
• Prices: $249.00, $1,025.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 865362-74-9
• Chemical Name: 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
• Formula: C18H13N7
• Molecular Weight: 327.34
• Purity: >98 %
• Description: Selective ERK inhibitor (IC 50 values are 0.14 and 0.31 μ M for ERK2 and ERK1 respectively). Displays 30-fold selectivity for ERK over p38 α (IC 50 = 10 μ M); displays no activity against human recombinant MEK1, MKK4, IKK α , PKC α , Src, Syc and PDGF α at concentrations less than 30 μ M. Also inhibits TGF β -induced AP-1 activation in Mv1Lu cells (IC 50 = 3.1 μ M).

Product References

Identification of a selective ERK inhibitor and structural determination of the - Identification of a selective ERK inhibitor and structural determination of the

Ohori M, Kinoshita T, Okubo M, Sato K, Yamazaki A, Arakawa H, Nishimura S, Inamura N, Nakajima H, Neya M, Miyake H, Fujii T. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63.

Signaling to extracellular signal-regulated kinase from ErbB1 kinase and protein - Signaling to extracellular signal-regulated kinase from ErbB1 kinase and protein

Perrett RM, Fowkes RC, Caunt CJ, Tsaneva-Atanasova K, Bowsher CG, McArdle CA. J Biol Chem. 2013 Jul 19;288(29):21001-14.