RIG012

• CAT Number: I041776
• CAS Number: 2642218-43-5
• Molecular Formula: C23H21NO3
• Molecular Weight: 359.42
• Purity: ≥95%
• Synonyms: 3,3-diethyl-4-phenylmethoxybenzo[g]indole-2,5-dione
• InChI: InChI=1S/C23H21NO3/c1-3-23(4-2)18-19(24-22(23)26)16-12-8-9-13-17(16)20(25)21(18)27-14-15-10-6-5-7-11-15/h5-13H,3-4,14H2,1-2H3
• InChIKey: OEWZCENSPLZNPQ-UHFFFAOYSA-N
• SMILES: CCC1(C2=C(C(=O)C3=CC=CC=C3C2=NC1=O)OCC4=CC=CC=C4)CC

RIG012 is a potent RIG-I inhibitor with an IC50 of 0.71 μM using the NADH-coupled ATPase assay. RIG012 inhibits IFN-β and ISG hRsad2 expression[1].
RIG012 contains a strong chromophore that absorbs in the visible range (λmax of 470 nm). Upon binding to RIG-I, the 470 nm absorbance band of RIG012 undergoes a dramatic hyperchromic shift to higher intensity values[1].
RIG012 (1, 1.25, 1.5, 2, 2.5, 3, 4 μM) has potent, dose-dependent inhibition of RIG-I signaling in HEK293T cells cotransfected with expression and reporter plasmids[1].
RIG012 (1.25, 2.25, 4.5, 9, 18 μM) has a potent, dose-dependent inhibition of IFN-β and ISG hRsad2 expression in A549 cells[1].

Reference

[1]. David C Rawling, et al. Small-Molecule Antagonists of the RIG-I Innate Immune Receptor. ACS Chem Biol. 2020 Feb 21;15(2):311-317.
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