RU.521 | cGAS Inhibitor

RU.521 is an inhibitor of cyclic GMP-AMP synthase (cGAS), an important innate immune system sensor of foreign cytoplasmic double-stranded DNA.1,2 IC50 = 0.70 µM in dsDNA-stimulated RAW macrophages1 and ~0.80 µM in wild type human THP-1 cells2. It is selective for cGAS with no targeting of IFNB1 protein, interferon receptors, or downstream signaling components of the JAK/STAT pathway. RU.521 was able to significantly increase cardiac output in a mouse model of sepsis.3 Active in both mouse and human cell lines.

  1. Vincent et al. (2017), Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice; Nat. Commun. 8 750
  2. Wiser et al. (2020), Small molecule inhibition of human cGAS reduces total cGAMP output and cytokine expression in cells; Sci. Rep. 10 7604
  3. Xu et al. (2020), Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice; Life Sci. 260 118315
Weight N/A
Dimensions N/A
Size:

5 mg, 25 mg

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CAS:
2262452-06-0
Catalog Number:
10-4140
Activity:
cGAS Inhibitor
Chemical Name:

3-[1-(6,7-Dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methylpyrazol-4-yl]-3H-isobenzofuran-1-one

Molecular Weight:
415.23
Molecular Formula:
C19H12Cl2N4O3
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white to pale pink solid
Purity:
>98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

RU.521 | cGAS Inhibitor

$95.00$325.00

CAS:
2262452-06-0
Catalog Number:
10-4140
Activity:
cGAS Inhibitor
Chemical Name:

3-[1-(6,7-Dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methylpyrazol-4-yl]-3H-isobenzofuran-1-one

Molecular Weight:
415.23
Molecular Formula:
C19H12Cl2N4O3
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white to pale pink solid
Purity:
>98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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