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SMIFH2 is an inhibitor of formin homology 2 (FH2) domains.1 It inhibits assembly of profilin-actin mediated by mouse formin mDia1(FH1FH2) with an IC50 value of approximately 15 μM. It also inhibits actin assembly mediated by FH1FH2 constructs of mDia2, C. elegans CYK-1, S. pombe Cdc12 or Fus1, or S. cerevisiae Bni1. SMIFH2 (25 μM) disassembles formin-dependent actin cables and contractile rings, but not Arp2/3-dependent actin patches, in fission yeast. It is cytotoxic to NIH3T3 fibroblasts (IC50 = 28 μM). SMIFH2 (10 μM) increases and decreases the percentage of NIH3T3 cells with thin and thick F-actin bundles, respectively.
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1. Identification and characterization of a small molecule inhibitor of formin-