纯度:>98% by HPLC,;NMR (Conforms)
分子式:C27H27N7O2S
分子量:513.62
溶剂:DMSO (10 mg/ml with warming)
性状:Off-white solid
存储:RT
Activity (short version):RNA polymerase I inhibitor
Function / Pharmacology:CX-5461 (1138549-36-6) is a first-in-class selective RNA polymerase I inhibitor, suppressing Pol I transcription in MV 4;11 myelomonocytic leukemia cells and SR immunoblastic lymphoma cells with EC50 values of 95 and 135 nM respectively and demonstrating 200-fold selectivity over Pol II.1,2 Activates the DNA damage response.3 It induces a rapid accumulation of cytosolic DNA which results in upregulation of STING.4 Acts as a potent immunosuppressant inhibiting T cell-mediated alloimmunity and representing a novel class of immunosuppressant.5