CX-5461, RNA polymerase I inhibitor

Product Details

Formal 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

Molecular Formula: C₂₇H₂₇N₇O₂S

Formula Weight: 513.6

CAS Number: 1138549-36-6

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to 10 mg/ml with warming)

Storage: RT

Stability: ≥ 2 years.

Applications

RNA polymerase I inhibitor

Functions

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. Activates the DNA damage response. It induces a rapid accumulation of cytosolic DNA which results in upregulation of STING. Acts as a potent immunosuppressant inhibiting T cell-mediated alloimmunity and representing a novel class of immunosuppressant.

Application Procedures

First dissolved in DMSO (10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)