A cGAS inhibitor
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RU-521

Item No. 31765

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    RU-521 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50 = 0.11 µM).1 It inhibits dsDNA-, but not IFN-β- or 5'ppp-HP20 RNA-, induced IFN-β1-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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vincent, J., Adura, C., Gao, P., et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat. Commun. 8(1), 750 (2017).