RU-521

RU-521 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS, IC50 = 0.11 µM). It inhibits dsDNA-, but not IFN-beta- or 5'ppp-HP20 RNA-, induced IFN-beta1-dependent gene expression in reporter assays and does not inhibit Pam3CSK4-, poly(I:C)-, or LPS-induced Il6 mRNA expression in RAW 264.7 cells, indicating selectivity for cGAS-mediated signaling. It reduces basal Ifnb1 mRNA expression in bone marrow-derived macrophages (BMDMs) generated from the Trex1-/- mouse model of Aicardi-Goutières syndrome, an autoimmune disorder characterized by constitutive activation of cGAS and IFN overproduction.Formal Name: 3-[1-(6,7-dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl]-1(3H)-isobenzofuranone. CAS Number: 2262452-06-0. Synonyms: RU-320521. Molecular Formula: C19H12Cl2N4O3. Formula Weight: 415.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 303 nm. SMILES: O=C1OC(C2=C(N(C3=NC4=C(N3)C(Cl)=C(Cl)C=C4)N=C2C)O)C5=C1C=CC=C5. InChi Code: InChI=1S/C19H12Cl2N4O3/c1-8-13(16-9-4-2-3-5-10(9)18(27)28-16)17(26)25(24-8)19-22-12-7-6-11(20)14(21)15(12)23-19/h2-7,16,26H,1H3,(H,22,23). InChi Key: VIQXILLOJLATEF-UHFFFAOYSA-N.