328007

Sigma-Aldrich

ERK Inhibitor II, FR180204 - CAS 865362-74-9 - Calbiochem

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; Ki = 310 nM and 140 nM, respectively).

Synonym(s):
5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine, ERK Inhibitor II, FR180204 - CAS 865362-74-9 - Calbiochem
Empirical Formula (Hill Notation):
C18H13N7
CAS Number:
Molecular Weight:
327.34
MDL number:

storage conditions

+2C to +8C

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC50 = 510 nM and 330 nM; Ki = 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).
A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC50 = 510 nM and 330 nM; Ki = 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).

Packaging

1 mg in Plastic ampoule
Packaged under inert gas

Biochem/physiol Actions

Target IC50: 510 nM and 330 nM
Target Ki: 310 nM and 140 nM, against ERK1 and ERK2, respectively
Cell permeable: yes
Reversible: no
Product competes with ATP.
Primary Target
ERK1 and ERK2

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Certificate of Analysis

Certificate of Origin

G Ruiz-Heiland et al.
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