A cell-permeable thiooxodihydropyrimidinedione compound that inhibits both formin-mediated, profilin-independent actin nucleation (IC₅₀ ~15 µM using mDia1 or mDia2) and formin-mediated elongation of actin filaments in the presence of profilin (IC₅₀ ~4 µM using Cdc12 or mDia2), but not the Arp2/3-mediated or formin-independent actin assembly. SMIFH2 targets the FH2 (formin homology 2) domain of formins from a large variety of species, including murine mDia1/2, C. elegans CYK-1, S. pombe Cdc12, S. pombe Fus1, and S. cerevisiae Bni1, and decreases formin affinity for the actin filament barbed end. SMIFH2, at 25 µM, is shown to selectively disrupt formin-dependent actin cables and contractile rings, but not Arp2/3-dependent, CK-666- (Cat. No. 182515) sensitive actin patches, in fission yeast. SMIFH2 is also demonstrated to affect F-actin cytoskeleton structures and cell migration (by a 2-fold decrease at 10 µM) in NIH 3T3 fibroblast cultures.

Packaged under inert gas

Toxicity: Standard Handling (A)

Use only fresh DMSO. Following reconstiution, aliquot an freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Rizvi, S.A., et al. 2009. Chem. Biol.16, 1158.

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