328007

ERK Inhibitor II, FR180204

ERK Inhibitor II, FR 180204, CAS 865362-74-9, is a cell-permeable, potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC₅₀ = 510 nM and 330 nM; K_i = 310 nM and 140 nM, respectively).

• Sinônimo(s): ERK Inhibitor II, FR180204, 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
• Fórmula empírica (Notação de Hill): C₁₈H₁₃N₇
• Número CAS: 865362-74-9
• Peso molecular: 327.34
• Número MDL: MFCD14585805
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
• chave InChI: XVECMUKVOMUNLE-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC₅₀ = 510 nM and 330 nM; K_i = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC₅₀ = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC₅₀ = 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008). Also available as a 10 mM solution in DMSO (Cat. No. 328010).

A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC₅₀ = 510 nM and 330 nM; K_i = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC₅₀ = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC₅₀ of 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008). Also available in InSolution format (Cat. No. 328010).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
ERK1 and ERK2

Product competes with ATP.

Reversible: no

Target IC₅₀: 510 nM and 330 nM

Target K_i: 310 nM and 140 nM, against ERK1 and ERK2, respectively

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Ohori, M., et al. 2005. Biochem. Biophys. Res. Commun.336, 357.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable