Chemical Structure : XL-3158
CAS No.:
XL-3158
(XL3158)
Catalog No.: PC-24705Not For Human Use, Lab Use Only.
XL-3158 is a potent, selective, cross-species, allosteric inhibitor of cyclic GMP-AMP synthase (cGAS), has binding affinity to the catalytic domain of human cGAS (h-cGASCD) with a Kd of 7.19 μM, effectively inhibits cGAS-DNA condensate formation.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
XL-3158 is a potent, selective, cross-species, allosteric inhibitor of cyclic GMP-AMP synthase (cGAS), has binding affinity to the catalytic domain of human cGAS (h-cGASCD) with a Kd of 7.19 μM, effectively inhibits cGAS-DNA condensate formation.
XL-3158 inhibits cGAS phase separation in cells.
XL-3158 exhibits an IC50 value of 11.1 μM against h-cGAS and EC0 of 11.85 μM in cellular assays.
XL-3158 potently inhibits cGAS in murine species with IC50 and EC50 values of 2.19 μM and 2.67 μM, respectively, in recombinant m-cGAS and RAW-ISG cells, but not G150.
XL-3158 (25 mg/kg, i.p.) attenuates cerulein-induced acute pancreatitis.
Physicochemical Properties
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M.Wt
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690.61
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Formula
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C30H17F7N6O2S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4,4'-((4-(trifluoromethyl)phenyl)methylene)bis(1-(4,6-difluorobenzo[d]thiazol-2-yl)-3-methyl-1H-pyrazol-5-ol)
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References
1. Zhao W, et al. Nat Commun. 2025 Jun 3;16(1):5140.
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