PKC_βII/EGFR Inhibitor

A cell-permeable symmetrical phthalimide compound that acts as a potent, reversible, and ATP-competitive inhibitor of EGFR and PKC isozymes α, βI, and βII (IC₅₀ = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM against EGFR and PKC isozymes α, βI, and βII, respectively

Packaged under inert gas

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

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Perrotti, D., et al. 1998. EMBO J.17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol.10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res.1, 813.
Trinks, U., et al. 1994. J. Med. Chem.37, 1015.

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

Toxicity: Standard Handling (A)