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Key Documents

328010

Sigma-Aldrich

ERK Inhibitor II, FR180204

InSolution, ≥97%

Synonym(s):

InSolution ERK Inhibitor II, FR180204

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About This Item

Empirical Formula (Hill Notation):
C18H13N7
Molecular Weight:
327.34
UNSPSC Code:
12352200

Quality Level

100

Assay

≥97% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

shipped in

wet ice

storage temp.

−20°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 (Cat. No. 328008) and the solid form of this compound (Cat. No. 328007) are also available..
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).

Packaging

Packaged under inert gas

Physical form

A 10 mM (500 µg/153 µl) solution of ERK Inhibitor II, FR180204 (Cat. No. 328007) in DMSO.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

Storage Class Code

10 - Combustible liquids

WGK

WGK 2

Flash Point(F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Flash Point(C)

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

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Sarit Cohen-Kedar et al.
European journal of immunology, 51(4), 864-878 (2021-02-23)
Intestinal epithelial cells (IECs) are the first to encounter luminal antigens and play an active role in intestinal immune responses. We previously reported that β-glucans, major fungal cell-wall glycans, induced chemokine secretion by IEC lines in a Dectin-1- and Syk-dependent

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