SW393109

SW393109 potently inhibits the kinase activity of the purified intact CDK8 kinase module in vitro, with an IC₅₀ of 3.16 nM^[1].
SW393109 induces the EWSR1::FLI1-repressed DKK1-nLuc reporter gene in A-673 EF-SMASh; DKK1-nLuc Ewing sarcoma cells, with an EC₅₀ of 5 nM^[1].
SW393109 (3-300 nM) fully inhibits IFNγ-induced STAT1^S727 phosphorylation in A-673 Ewing sarcoma cells at high concentrations, while only partially inhibits this process at low concentrations^[1].
SW393109 (100 nM; 24 h) alters the EWSR1::FLI1 transcriptional program in A-673 and TC-32 Ewing sarcoma cells, with gene expression changes consistent with those induced by targeted inhibition of CDK8^[1].
SW393109 (0.0001-10 μM; 4-5 days) inhibits the proliferation of A-673 and TC-32 Ewing sarcoma cells, and selective sensitivity is observed in cell lines driven by transcription fusion oncoproteins^[1].
SW393109 (100 nM; 24 h) induces sequestration of the CDK8 kinase module with the core mediator complex in A-673 Ewing sarcoma cells, thereby enhancing the stability and binding of the complex^[1].
SW393109 (100 nM; 24 h) induces global chromatin retention of the CDK8 kinase module and core mediator complex in A-673 Ewing sarcoma cells, with enhanced retention at regions containing a single GGAA motif^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.