STAT3-IN-52 is a selective inhibitor of signal transducer and activator of transcription 3 (STAT3) that acts by binding to the phosphorylated tyrosine 705 (pY705) site, with a Ki value of 440 nM. This compound effectively blocks the phosphorylation and dimerization of STAT3, leading to cytotoxic effects in various cancer cell lines, including MDA-MB-231 breast cancer cells (IC50 = 0.7 μM), UW426 medulloblastoma, and BKPC3 pancreatic cancer cells. Additionally, STAT3-IN-52 induces apoptosis, inhibits STAT3 nuclear transport and DNA binding, and downregulates the expression of the STAT3 target gene MMP9, making it a valuable reagent for studying STAT3 dysregulation in cancer research.
STAT3-IN-52 is a selective inhibitor of signal transducer and activator of transcription 3 (STAT3) that acts by binding to the phosphorylated tyrosine 705 (pY705) site, with a Ki value of 440 nM. This compound effectively blocks the phosphorylation and dimerization of STAT3, leading to cytotoxic effects in various cancer cell lines, including MDA-MB-231 breast cancer cells (IC50 = 0.7 μM), UW426 medulloblastoma, and BKPC3 pancreatic cancer cells. Additionally, STAT3-IN-52 induces apoptosis, inhibits STAT3 nuclear transport and DNA binding, and downregulates the expression of the STAT3 target gene MMP9, making it a valuable reagent for studying STAT3 dysregulation in cancer research.
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