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).

• Synonyme(s) : ERK Inhibitor II, FR180204, 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
• Formule empirique (notation de Hill): C₁₈H₁₃N₇
• Numéro CAS: 865362-74-9
• Poids moléculaire : 327.34
• Numéro MDL: MFCD14585805
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 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)
• Clé InChI: XVECMUKVOMUNLE-UHFFFAOYSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable