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Merck

328007

Sigma-Aldrich

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

Synonym(s):

ERK Inhibitor II, FR180204, 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine

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About This Item

Empirical Formula (Hill Notation):
C18H13N7
CAS Number:
865362-74-9
Molecular Weight:
327.34
MDL number:
MFCD14585805
UNSPSC Code:
12352200

Quality Level

100

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

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)

InChI key

XVECMUKVOMUNLE-UHFFFAOYSA-N

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 = 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; 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).

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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