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328008

Sigma-Aldrich

ERK Inhibitor II, Negative Control, FR180209

The ERK Inhibitor II, Negative Control, also referenced under CAS 1177970-73-8, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

ERK Inhibitor II, Negative Control, FR180209, 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ol, Chk2 Inhibitor IV, Irfin1, Insulin Receptor Family Inhibitor, Aurora Kinase Inhibitor XII

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About This Item

Empirical Formula (Hill Notation):
C18H12N6O
CAS Number:
Molecular Weight:
328.33
UNSPSC Code:
12352200

Quality Level

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

green

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C18H12N6O/c25-18-12-10-13(19-20-17(12)21-22-18)15-14-8-4-5-9-24(14)23-16(15)11-6-2-1-3-7-11/h1-10H,(H2,20,21,22,25)

InChI key

QMBDONCHHMIWFJ-UHFFFAOYSA-N

General description

A cell-permeable Erk Inhibitor II (Cat. No. 328007) structural analog that acts as a isoform-selective Aurora B kinase inhibitor (95% inhibition at 1 µM; [ATP] = 10 µM) with little or no activity against Aurora A or C (0% and 16% inhibition, respectively, at 1 µM; [ATP] = 15 µM), Also shown to inhibit Chk2, IRR/INSRR, and Ack1/TNK2 (% inhibition/[ATP] = 81%/70 µM, 75%/200 µM, and 71%/70 µM, respectively), while exhibiting much reduced or no inhibitory potency toward a panel of 228 other kinases, including Erk1/2.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Aurora B kinase
Product does not compete with ATP.
Reversible: no
Target IC50: 95% inhibition at 10 µM using 1 µM; [ATP]

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Anastassiadis, T., et al. 2013. J. Biol. Chem.288, In press.
Gao, Y., et al. 2013. Biochem. J.in press.
Ohori, M., et al. 2005. Biochem. Biophys. Res. Commun.336, 357.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

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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