Chemical Name: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-5H-benzothiazolo [3,2-a][1,8]naphthyridine-6-carboxamide
RNA polymerase I inhibitor
Molecular Weight:
513.62
Purity:
>98% by HPLC, NMR (Conforms)
Form:
Off-white solid
CAS Number:
[1138549-36-6]
Formula:
C27H27N7O2S
Application Notes:
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
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