3117797-77-7
Chemical Structure
XL-3158
- CAS No.: 3117797-77-7
- Formula:C30H17F7N6O2S2
- Molecular Weight:690.61
InChIKey: LMARGMCGTTZFIP-UHFFFAOYSA-N
SMILES: CC1=NN(C(O)=C1C(C2=C(N(N=C2C)C3=NC4=C(S3)C=C(C=C4F)F)O)C5=CC=C(C(F)(F)F)C=C5)C6=NC7=C(S6)C=C(C=C7F)F
Biological Activity: XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases[1].
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XL-3158 | 99.55% | XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases. | ||||||||||||||||||||
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Keywords
